2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis Autophagy
  3. EGFR Ferroptosis Autophagy
  4. Lapatinib tosylate

Lapatinib tosylate  (Synonyms: GW572016 tosylate; GW2016 tosylate)

目录号: HY-50898C
产品使用指南

摩尔计算器

Lapatinib (GW572016) tosylate 是一种有效的，具有口服活性的 ErbB-2 和 EGFR 酪氨酸激酶结构域的抑制剂，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 tosylate Chemical Structure

Lapatinib tosylate Chemical Structure

CAS No. : 1187538-35-7

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Lapatinib tosylate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 68 篇科研文献

WB

    Lapatinib tosylate 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 tosylate 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 tosylate 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 tosylate 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 tosylate 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 tosylate 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+PIK3CAH1047R tumors treated as indicated. Transplants of NIC+PIK3CAH1047R 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 tosylate 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 tosylate 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.

    查看 EGFR 亚型特异性产品:

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    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Lapatinib (GW572016) tosylate is a potent, orally active 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)

    ErbB2

    9.8 nM (IC50)

    体外研究
    (In Vitro)

    Lapatinib (GW2016; 0.03-10 µM; 6 hours; BT474 and HN5 cells) tosylate treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner[1].
    Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) tosylate treatment has a selective inhibition of the proliferation of human tumor cell lines[1].
    Lapatinib (GW2016; 1-10 µM; 72 hours; HN5 cells) treatment results in induces G1 arrest[1].

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

    Lapatinib tosylate 相关抗体:

    Cell Proliferation Assay[1]

    Cell Line: HN5, A-43, BT474, N87, and CaLu-3 cells
    Concentration: 1 nM-100 µM
    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.

    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.
    体内研究
    (In Vivo)

    Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) tosylate treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose[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

    753.26

    Formula

    C36H34ClFN4O7S2
    CAS 号
    中文名称

    甲苯磺酸拉帕替尼
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Lapatinib tosylate 相关分类

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    • 稀释计算器

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    • 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:

    Lapatinib1187538-35-7GW572016GW2016甲苯磺酸拉帕替尼GW 572016GW-572016GW 2016GW-2016EGFRFerroptosisAutophagyEpidermal growth factor receptorErbB-1HER1orally activeErbB-2anticancer effectInhibitorinhibitorinhibit

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