Lapatinib (Synonyms: 拉帕替尼; GW572016; GW2016)

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摩尔计算器

Lapatinib (GW572016) 是一种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC₅₀ 值分别为 10.2 和 9.8 nM。

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Lapatinib Chemical Structure

CAS No. : 231277-92-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥770	In-stock
50 mg	￥700	In-stock
100 mg	￥1200	In-stock
500 mg	￥3000	In-stock
1 g	￥4500	In-stock
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Other Forms of Lapatinib:

Lapatinib-d₄ In-stock
Lapatinib ditosylate In-stock
Lapatinib ditosylate monohydrate In-stock
Lapatinib-d7 ditosylate 询价
Lapatinib-d₇ dihydrochloride 询价
Lapatinib-d₅ 询价
Lapatinib-d₄-1 询价
Lapatinib tosylate 询价
Lapatinib (Standard) 询价

MCE 顾客使用本产品发表的 70 篇科研文献

: Lapatinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):123. [Abstract]; MCF-7 cells are treated with or without 5 μg/mL cisplatin (DDP) for 48 h after preincubated with or without Lapatinib at the indicated concentrations for 6 h, respectively. Then the levels of ER-α36, total EGFR and P-EGFR, total HER-2 and P-HER-2, total ERK and P-ERK are evaluated using western blot.

: Lapatinib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]; Immunoblot analysis of U-CH1 cells treated with the indicated doses of inhibitors (Afatinib, Erlotinib and Lapatinib) for 2 h (upper panel) or 48 h (lower panel). Protein cell extracts are resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC₅₀s of the different inhibitors are reported.

: Lapatinib purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2018 Sep;82(3):383-394. [Abstract]; The expression level of EGFR and HER2 on normal esophageal epithelium cell and four esophageal squamous cancer cell lines analyzed by western blot.

: Lapatinib purchased from MCE. Usage Cited in: Nature. 2017 Aug 24;548(7668):471-475. [Abstract]; Western blot of SKBR3, BT474, MDA-MB-453, and MDA-MB-361 cells treated with DMSO, Lapatinib, or Abemaciclib for 48 h. Western blot of MDA-MB-453 cells pretreated with DMSO or Abemaciclib (500 nM) for 0, 1, or 7 days before exposure to Staurosporine (500 nM) for 4 h.

: Lapatinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Aug 24;8(62):104894-104912. [Abstract]; MDA-MB-231 cells are serum-starved overnight and pre-treated with 3 μM Lapatinib or DMSO for 3 hours. After that time, cells are lysed (0hr) or stimulated with EGF for 1, 8, 24, 48, and 72 hours. Western blots of p-EGFR (Tyr1173), EGFR, p-cJun (ser63), cJun, and vinculin are shown with band densitometries beneath.

: Lapatinib purchased from MCE. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]; Western blot analysis of p-AKT(T308), p-AKT(S473) and p-ERK in transplanted NIC⁺PIK3CA^H1047R tumors treated as indicated. Transplants of NIC⁺PIK3CA^H1047R primary mammary tumors are first established in immunodeficient nude mice maintained on Doxycycline. Treatment starts when tumor transplants reach 500 mm³. DOX On, on Doxycycline; DOX Off, Doxycycline withdrawal. Lapatinib, 100mg/kg/day, p.o; GDC-0941, 120mg/kg/ day, p.o. Tumo

: Lapatinib purchased from MCE. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]; The combined use of MEK162 with HER kinase inhibitor Lapatinib, almost completely abolishes MAPK signaling as evidenced by diminished phospho-Erk levels. Western blot analyses of ERK signaling in tumor transplants from mice treated as indicated. Three hours after their dose on day four of treatment, the mice are sacrificed for analysis. Vinculin is used as a loading control.

: Lapatinib purchased from MCE. Usage Cited in: Tumour Biol. 2016 Nov;37(11):14831-14839. [Abstract]; Western blot analysis of PI3K signaling in cell lysates treated with Lapatinib (1 μM) with or without BYL719.

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生物活性
纯度 & 产品资料
参考文献

生物活性

Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively^[1].

IC₅₀ & Target^[1]

EGFR

10.2 nM (IC₅₀, Cell Free Assay)

ErbB2

9.8 nM (IC₅₀, Cell Free Assay)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
3T3	EC₅₀	13 μM Compound: 1	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay	[PMID: 28337329]
A2780	IC₅₀	10.4 μM Compound: Lapatinib	Antiproliferative activity against human A2780 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
A2780	IC₅₀	10.4 μM Compound: Lapatinib	Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay	[PMID: 29684708]
A-431	IC₅₀	> 10000 nM Compound: Lapatinib	Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA	[PMID: 20346655]
A-431	IC₅₀	0.15 μM Compound: 3; GW-572016	Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
A-431	IC₅₀	0.97 μM Compound: 5, GW-572016	Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay	[PMID: 21080629]
A-431	IC₅₀	104 nM Compound: 1	Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay	[PMID: 22372864]
A-431	IC₅₀	104 nM Compound: 3	Cytotoxicity against human A431 cells after 72 hrs by SRB assay Cytotoxicity against human A431 cells after 72 hrs by SRB assay	[PMID: 19888761]
A-431	IC₅₀	2.6 μM Compound: 3	Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay	[PMID: 22595177]
A-431	IC₅₀	2.62 μM Compound: Lapatinib	Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay	[PMID: 22182581]
A-431	IC₅₀	2.66 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells after 72 hrs by MTT assay Antiproliferative activity against human A431 cells after 72 hrs by MTT assay	[PMID: 30508379]
A-431	IC₅₀	3.59 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells overexpressing EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human A431 cells overexpressing EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 29421573]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 28711703]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition by MTT assay	[PMID: 32739648]
A-431	IC₅₀	52 nM Compound: Lapatinib	Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA	[PMID: 20346655]
A-431	IC₅₀	643.1 nM Compound: Lapatinib	Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
A549	IC₅₀	0.51 μM Compound: 3; GW-572016	Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
A549	IC₅₀	11 μM Compound: Tykerb(R)	Antiproliferative activity against human A549 cells overexpressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells overexpressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
A549	IC₅₀	11.3 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay	[PMID: 32739648]
A549	IC₅₀	13.26 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay	[PMID: 32739648]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay	[PMID: 29421573]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay	[PMID: 28711703]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition by MTT assay	[PMID: 32739648]
A549	IC₅₀	3.64 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30508379]
A549	IC₅₀	6.74 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 27187856]
A549	IC₅₀	8.5 μM Compound: 5, GW-572016	Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay	[PMID: 21080629]
AU565	IC₅₀	0.064 μM Compound: Lapatinib	Antiproliferative activity against human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
B16-F10	IC₅₀	0.21 μM Compound: Lapatinib	Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay	[PMID: 26652482]
Bel-7402	IC₅₀	3.7 μM Compound: Lapatinib	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 28092860]
BT-474	IC₅₀	0.025 μM Compound: lapatinib	Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method	[PMID: 21887403]
BT-474	IC₅₀	0.031 μM Compound: Lapatinib	Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay	[PMID: 27288180]
BT-474	IC₅₀	0.037 μM Compound: Lapatinib	Antiproliferative activity against human BT474 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human BT474 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
BT-474	IC₅₀	0.064 μM Compound: Lapatinib	Antiproliferative activity against human BT474 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human BT474 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
BT-474	IC₅₀	0.08 μM Compound: 1, GW-572016	Inhibition of BT474 cell growth after 72 hrs Inhibition of BT474 cell growth after 72 hrs	[PMID: 16777410]
BT-474	IC₅₀	0.1 μM Compound: Lapatinib	Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining	[PMID: 22101132]
BT-474	IC₅₀	0.1 μM Compound: 3; GW-572016	Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
BT-474	GI₅₀	0.2 μM Compound: Lapatinib	Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
BT-474	GI₅₀	0.93 μM Compound: Lapatinib	Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay	[PMID: 26475520]
BT-474	IC₅₀	140 nM Compound: Lapatinib	Inhibition of ERBb2 phosphorylation in human BT474 cells by ELISA Inhibition of ERBb2 phosphorylation in human BT474 cells by ELISA	[PMID: 20817523]
BT-474	IC₅₀	63.9 nM Compound: Lapatinib	Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
CAL-27	IC₅₀	< 32 nM Compound: 5, GW-572016	Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot	[PMID: 21080629]
CAL-27	IC₅₀	0.007 μM Compound: 5, GW-572016	Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay	[PMID: 21080629]
CAL-27	IC₅₀	0.53 μM Compound: 5, Tykerb	Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
Calu-3	IC₅₀	0.1 μM Compound: Lapatinib	Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay	[PMID: 28092860]
Calu-3	IC₅₀	0.216 μM Compound: Lapatinib	Antiproliferative activity against human Calu3 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human Calu3 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
Calu-3	IC₅₀	0.23 μM Compound: Lapatinib	Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
CAMA-1	IC₅₀	> 10 μM Compound: Lapatinib, Tykerb	Antiproliferative activity against human progesterone receptor and HER2 deficient CAMA1 cells expressing estrogen receptor after 72 hrs by MTT assay Antiproliferative activity against human progesterone receptor and HER2 deficient CAMA1 cells expressing estrogen receptor after 72 hrs by MTT assay	[PMID: 23927972]
COLO 205	IC₅₀	4.6 μM Compound: Lapatinib	Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay	[PMID: 28092860]
CWR22R	IC₅₀	6.06 μM Compound: 5, Tykerb	Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
DU-145	IC₅₀	2.99 μM Compound: 5, Tykerb	Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
DU-145	GI₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
EOL1	GI₅₀	0.41 μM Compound: Lapatinib	Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
HCC1954	IC₅₀	5 μM Compound: Tykerb(R)	Antiproliferative activity against human HCC1954 cells overexpressing HER2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC1954 cells overexpressing HER2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
HCC827	IC₅₀	0.6 μM Compound: Lapatinib	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
HCC827	IC₅₀	0.6 μM Compound: Lapatinib	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay	[PMID: 29421573]
HCC827	GI₅₀	22.3 μM Compound: Lapatinib	Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
HCT-116	IC₅₀	10.12 μM Compound: Lapatinib	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 29684708]
HCT-116	IC₅₀	12 nM Compound: Lapatinib	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 33545637]
HCT-116	IC₅₀	13.14 μM Compound: 5, Tykerb	Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
HCT-116	GI₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
HCT-116	IC₅₀	42.36 μM Compound: 3	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 21570843]
HCT-116	IC₅₀	5.92 μM Compound: Lapatinib	Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay	[PMID: 30096580]
HCT-116	IC₅₀	5.92 μM Compound: Lapatinib	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay	[PMID: 32361329]
HCT-116	IC₅₀	6.2 μM Compound: Lapatinib	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28092860]
HEK-293T	CC₅₀	123.17 μM Compound: Lapatinib	Cytotoxicity against human HEK293T cells for 24 hrs by MTT assay Cytotoxicity against human HEK293T cells for 24 hrs by MTT assay	[PMID: 26652482]
HeLa	IC₅₀	0.12 μM Compound: Lapatinib	Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay	[PMID: 26652482]
HeLa	IC₅₀	5.9 μM Compound: 5, GW-572016	Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay	[PMID: 21080629]
Hep 3B2	IC₅₀	5.49 μM Compound: lapatinib	Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay	[PMID: 20143778]
HepG2	IC₅₀	0.27 μM Compound: Lapatinib	Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay	[PMID: 26652482]
HepG2	IC₅₀	11.71 μM Compound: Lapatinib	Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay	[PMID: 30096580]
HepG2	IC₅₀	11.71 μM Compound: Lapatinib	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by SRB assay	[PMID: 32361329]
HepG2	IC₅₀	6.27 μM Compound: lapatinib	Antiproliferative activity against human HepG2 cells after hrs by ATP content assay Antiproliferative activity against human HepG2 cells after hrs by ATP content assay	[PMID: 20143778]
HN5	IC₅₀	0.01 μM Compound: Lapatinib	Inhibition of EGF-induced EGFR phosphorylation at Tyr-residue in human HN5 cells preincubated for 24 hrs followed by EGF-stimulation and measured after 15 mins by Western blot analysis Inhibition of EGF-induced EGFR phosphorylation at Tyr-residue in human HN5 cells preincubated for 24 hrs followed by EGF-stimulation and measured after 15 mins by Western blot analysis	[PMID: 30600149]
HN5	IC₅₀	0.12 μM Compound: 1, GW-572016	Inhibition of HN5 cell growth after 72 hrs Inhibition of HN5 cell growth after 72 hrs	[PMID: 16777410]
HS27	IC₅₀	> 10000 nM Compound: 3	Cytotoxicity against human HS27 cells after 72 hrs by SRB assay Cytotoxicity against human HS27 cells after 72 hrs by SRB assay	[PMID: 19888761]
HT-29	IC₅₀	12.67 μM Compound: Lapatinib	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
HT-29	IC₅₀	4.62 μM Compound: 5, Tykerb	Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
HT-29	IC₅₀	6.81 μM Compound: Lapatinib	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay	[PMID: 32739648]
HT-29	IC₅₀	8.85 μM Compound: Lapatinib	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay	[PMID: 32739648]
HUVEC	IC₅₀	47.31 μM Compound: Lapatinib	Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
JeKo-1	GI₅₀	5 μM Compound: Lapatinib	Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
JIMT-1	IC₅₀	> 10000 nM Compound: 1	Cytotoxicity against human JIMT1 cells expressing low HER-2 after 72 hrs by SRB assay Cytotoxicity against human JIMT1 cells expressing low HER-2 after 72 hrs by SRB assay	[PMID: 22372864]
K562	GI₅₀	5.7 μM Compound: Lapatinib	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
KB	IC₅₀	0.062 μM Compound: Lapatinib	Inhibition of EGFR in human KB cells assessed as reduction in EGF-stimulated EGFR phosphorylation preincubated for 1 hr followed by EGF stimulation and measured after 6 mins by ELISA Inhibition of EGFR in human KB cells assessed as reduction in EGF-stimulated EGFR phosphorylation preincubated for 1 hr followed by EGF stimulation and measured after 6 mins by ELISA	[PMID: 32139324]
KG-1a	IC₅₀	9.76 μM Compound: Lapatinib	Antiproliferative activity against human KG1a cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human KG1a cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
L929	IC₅₀	2.05 μM Compound: Lapatinib	Cytotoxicity against mouse L929 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against mouse L929 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 30508379]
LNCaP	IC₅₀	3.68 μM Compound: 5, Tykerb	Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MCF7	IC₅₀	0.011 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 25151582]
MCF7	IC₅₀	0.47 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay	[PMID: 26652482]
MCF7	IC₅₀	12.62 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MCF7	IC₅₀	15.71 μM Compound: lapatinib	Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	[PMID: 24355130]
MCF7	IC₅₀	15.79 μM Compound: lapatinib	Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	[PMID: 24355130]
MCF7	IC₅₀	19.22 μM Compound: lapatinib	Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	[PMID: 24355130]
MCF7	IC₅₀	21 nM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 33545637]
MCF7	IC₅₀	4.691 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30792101]
MCF7	IC₅₀	4.83 μM Compound: 5, Tykerb	Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MCF7	IC₅₀	5.02 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay	[PMID: 30096580]
MCF7	IC₅₀	5.02 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by SRB assay	[PMID: 32361329]
MCF7	IC₅₀	6.301 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
MCF7	IC₅₀	6.6 μM Compound: lapatinib	Antiproliferative activity against human MCF7 cells after hrs by ATP content assay Antiproliferative activity against human MCF7 cells after hrs by ATP content assay	[PMID: 20143778]
MCF7	IC₅₀	6.8 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
MCF7	IC₅₀	6.8 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 29684708]
MCF7	GI₅₀	8.1 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
MCF7	IC₅₀	8468 nM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MCF7	IC₅₀	95 μM Compound: Tykerb(R)	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
MDA-MB-231	IC₅₀	> 100 μM Compound: Lapatinib	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MDA-MB-231	IC₅₀	10.373 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
MDA-MB-231	IC₅₀	10.6 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	GI₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MDA-MB-231	IC₅₀	29.39 μM Compound: Lapatinib	Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	30.78 μM Compound: Lapatinib	Antiproliferative activity against drug-tolerant human MDA-MB-231/lapatinib cells assessed as CD44-positive cells measured after 24 hrs by MTT assay Antiproliferative activity against drug-tolerant human MDA-MB-231/lapatinib cells assessed as CD44-positive cells measured after 24 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	4.691 μM Compound: Lapatinib	Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay	[PMID: 30792101]
MDA-MB-231	IC₅₀	5.4 μM Compound: lapatinib	Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay	[PMID: 20143778]
MDA-MB-231	IC₅₀	5.86 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	7.7 μM Compound: 5, Tykerb	Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MDA-MB-361	IC₅₀	1029 nM Compound: 1	Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay	[PMID: 22372864]
MDA-MB-453	IC₅₀	0.19 μM Compound: Lapatinib	Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MDA-MB-453	IC₅₀	555 nM Compound: 1	Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay	[PMID: 22372864]
MDA-MB-468	IC₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay	[PMID: 28092860]
MDA-MB-468	IC₅₀	23.46 μM Compound: 3	Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay	[PMID: 21570843]
MEXF276L	IC₅₀	11.37 μM Compound: 5, Tykerb	Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MIA PaCa-2	GI₅₀	10 μM Compound: Lapatinib	Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MKN-45	IC₅₀	11.48 μM Compound: 5, Tykerb	Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MRC5	IC₅₀	> 100 μM Compound: Lapatinib	Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MRC5	IC₅₀	13.66 μM Compound: Lapatinib	Cytotoxicity against human MRC5 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
MV4-11	GI₅₀	10 μM Compound: Lapatinib	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
NCI-H1975	IC₅₀	> 1000 nM Compound: 3	Cytotoxicity against human NCI-H1975 cells after 24 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells after 24 hrs by MTT assay	[PMID: 19888761]
NCI-H1975	IC₅₀	> 1000 nM Compound: 1	Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by SRB assay Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by SRB assay	[PMID: 22372864]
NCI-H1975	IC₅₀	12.68 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
NCI-H1975	IC₅₀	12.68 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 29421573]
NCI-H1975	IC₅₀	7.25 μM Compound: 3; GW-572016	Antiproliferative activity against human NCI-H1975 expressing EGFR T790M/L858R mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1975 expressing EGFR T790M/L858R mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
NCI-H1975	IC₅₀	7.37 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
NCI-H1975	IC₅₀	9 μM Compound: Tykerb(R)	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
NCI-H1975	IC₅₀	9.08 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay	[PMID: 28711703]
NCI-H460	IC₅₀	> 100 μM Compound: Lapatinib	Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
NCI-H460	IC₅₀	13.46 μM Compound: 5, Tykerb	Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
NCI-H460	IC₅₀	8.4 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 28092860]
NCI-H522	IC₅₀	6.4 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay	[PMID: 28092860]
NCI-N87	IC₅₀	0.053 μM Compound: Lapatinib	Antiproliferative activity against human NCI-N87 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-N87 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
NCI-N87	IC₅₀	0.08 μM Compound: 1, GW-572016	Inhibition of N87 cell growth after 72 hrs Inhibition of N87 cell growth after 72 hrs	[PMID: 16777410]
NCI-N87	IC₅₀	0.09 μM Compound: Lapatinib	Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining	[PMID: 22101132]
NCI-N87	IC₅₀	100 nM Compound: Lapatinib	Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA	[PMID: 20346655]
NCI-N87	IC₅₀	36 nM Compound: 1	Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay	[PMID: 22372864]
NIH3T3	IC₅₀	4.3 μM Compound: 3	Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay	[PMID: 22595177]
OVCAR-3	IC₅₀	13.44 μM Compound: 5, Tykerb	Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
PANC-1	IC₅₀	8.12 μM Compound: 5, Tykerb	Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
PBMC	IC₅₀	28 μM Compound: lapatinib	Cytotoxicity against human PBMC assessed as induction of cell death by cell Titer-Glo assay Cytotoxicity against human PBMC assessed as induction of cell death by cell Titer-Glo assay	[PMID: 29909341]
PC-3M	IC₅₀	4.55 μM Compound: 5, Tykerb	Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
RAW264.7	EC₅₀	11 μM Compound: 1	Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay	[PMID: 28337329]
RKO	IC₅₀	5.35 μM Compound: 5, Tykerb	Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
SAOS-2	IC₅₀	9.38 μM Compound: 5, Tykerb	Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
SK-BR-3	IC₅₀	0.002 μM Compound: 5, GW-572016	Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay	[PMID: 21080629]
SK-BR-3	IC₅₀	0.017 μM Compound: GW-572016	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay	[PMID: 19028425]
SK-BR-3	IC₅₀	0.04 μM Compound: lapatinib	Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay	[PMID: 20143778]
SK-BR-3	IC₅₀	0.06 μM Compound: 3; GW-572016	Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
SK-BR-3	IC₅₀	0.49 μM Compound: Lapatinib	Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay	[PMID: 27187856]
SK-BR-3	IC₅₀	29 nM Compound: 1	Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay	[PMID: 22372864]
SK-BR-3	IC₅₀	29 nM Compound: 3	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay	[PMID: 19888761]
SK-BR-3	IC₅₀	30.1 nM Compound: Lapatinib	Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
SK-BR-3	IC₅₀	4.35 μM Compound: 3	Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay	[PMID: 21570843]
SK-BR-3	IC₅₀	4.4 μM Compound: Lapatinib	Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay	[PMID: 28092860]
SK-BR-3	IC₅₀	5.05 μM Compound: Lapatinib, Tykerb	Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay	[PMID: 23927972]
SK-BR-3	IC₅₀	9.76 μM Compound: Lapatinib	Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
SK-HEP1	IC₅₀	5.3 μM Compound: lapatinib	Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay	[PMID: 20143778]
SK-MEL19	GI₅₀	5 μM Compound: Lapatinib	Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-OV-3	IC₅₀	0.003 μM Compound: 5, GW-572016	Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay	[PMID: 21080629]
SK-OV-3	IC₅₀	0.59 μM Compound: Lapatinib	Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
SK-OV-3	IC₅₀	2.99 μM Compound: Lapatinib	Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay	[PMID: 22182581]
SUM-159-PT	IC₅₀	9.76 μM Compound: Lapatinib	Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human SW480 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 29421573]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 28711703]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay	[PMID: 32739648]
T-24	IC₅₀	9.65 μM Compound: 5, Tykerb	Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
T47D	IC₅₀	> 10 μM Compound: Lapatinib, Tykerb	Antiproliferative activity against human HER2 deficient T47D cells expressing estrogen receptor and progesterone receptor after 72 hrs by MTT assay Antiproliferative activity against human HER2 deficient T47D cells expressing estrogen receptor and progesterone receptor after 72 hrs by MTT assay	[PMID: 23927972]
T47D	GI₅₀	40 μM Compound: Lapatinib	Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
TE-671	IC₅₀	10.95 μM Compound: 5, Tykerb	Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
U-87MG ATCC	GI₅₀	10 μM Compound: Lapatinib	Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
WI-38	IC₅₀	> 10 μM Compound: GW-572016	Cytotoxicity against human WI38 cells after 72 hrs by SRB assay Cytotoxicity against human WI38 cells after 72 hrs by SRB assay	[PMID: 19028425]
WI-38	IC₅₀	45.2 nM Compound: Lapatinib	Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 33545637]

体外研究
(In Vitro)

Lapatinib (GW2016；0.03-10 μM；6 小时；BT474 和 HN5 细胞) 治疗以剂量反应方式抑制 EGFR 和 ErbB-2 受体自身磷酸化。Lapatinib 以剂量依赖性方式抑制 AKT 丝氨酸 473 的磷酸化^[1]。
Lapatinib (72小时；HN5、A-43、BT474、N87、和CaLu-3细胞) 治疗对人类肿瘤细胞系的增殖有选择性抑制作用^[1]。
Lapatinib（1-10 μM；72 小时；HN5 细胞）治疗导致 G1 停滞^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	BT474 and HN5 cells
Concentration:	0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, or 10 µM
Incubation Time:	6 hours
Result:	Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.

Cell Proliferation Assay^[1]

Cell Line:	HN5, A-43, BT474, N87, and CaLu-3 cells
Concentration:
Incubation Time:	72 hours
Result:	Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2.

Cell Cycle Analysis^[1]

Cell Line:	HN5 cells
Concentration:	1 µM, or 10 µM
Incubation Time:	72 hours
Result:	Resulted in induction of G1 arrest.

体内研究
(In Vivo)

Lapatinib（GW2016；30-100 mg/kg；口服；每日两次；连续 21 天；CD-1 雌性裸鼠）治疗在 30 和 100 mg/kg 时以剂量反应方式抑制 HN5 细胞的肿瘤异种移植生长，在较高剂量时完全抑制肿瘤生长^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CD-1 nude female mice (4-6 weeks old) with HN5 cells^[1]
Dosage:	30 mg/kg, 100 mg/kg
Administration:	Oral administration; twice daily; for 21 days
Result:	Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.

Clinical Trial

分子量

581.06

Formula

C₂₉H₂₆ClFN₄O₄S

CAS 号

231277-92-2

性状

固体

颜色

Light yellow to yellow

中文名称

拉帕替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 125 mg/mL (215.12 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7210 mL	8.6050 mL	17.2099 mL
5 mM	0.3442 mL	1.7210 mL	3.4420 mL
10 mM	0.1721 mL	0.8605 mL	1.7210 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.30 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.58 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案三

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.58 mM); 悬浊液; 超声助溶

此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案四

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.58 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 12% SBE-β-CD in Saline
Solubility: 5 mg/mL (8.60 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.83%

选择批次：

Data Sheet (643 KB) SDS (393 KB)

COA (192 KB) HNMR (197 KB) LCMS (475 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94 [Content Brief]

Lapatinib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7210 mL	8.6050 mL	17.2099 mL	43.0248 mL
	5 mM	0.3442 mL	1.7210 mL	3.4420 mL	8.6050 mL
	10 mM	0.1721 mL	0.8605 mL	1.7210 mL	4.3025 mL
	15 mM	0.1147 mL	0.5737 mL	1.1473 mL	2.8683 mL
	20 mM	0.0860 mL	0.4302 mL	0.8605 mL	2.1512 mL
	25 mM	0.0688 mL	0.3442 mL	0.6884 mL	1.7210 mL
	30 mM	0.0574 mL	0.2868 mL	0.5737 mL	1.4342 mL
	40 mM	0.0430 mL	0.2151 mL	0.4302 mL	1.0756 mL
	50 mM	0.0344 mL	0.1721 mL	0.3442 mL	0.8605 mL
	60 mM	0.0287 mL	0.1434 mL	0.2868 mL	0.7171 mL
	80 mM	0.0215 mL	0.1076 mL	0.2151 mL	0.5378 mL
	100 mM	0.0172 mL	0.0860 mL	0.1721 mL	0.4302 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lapatinib231277-92-2GW572016 GW2016拉帕替尼GW 572016GW-572016GW2016GW 2016GW-2016EGFRAutophagyFerroptosisEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Lapatinib (Synonyms: 拉帕替尼; GW572016; GW2016)

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MCE 顾客使用本产品发表的 70 篇科研文献

Lapatinib 相关产品

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Lapatinib (Synonyms: 拉帕替尼; GW572016; GW2016)

Customer Review

Other Forms of Lapatinib:

Lapatinib 相关抗体

MCE 顾客使用本产品发表的 70 篇科研文献

Lapatinib 相关产品

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