Ceritinib (Synonyms: 色瑞替尼; LDK378)

目录号: HY-15656 纯度: 99.98%: FAQs
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Ceritinib (LDK378) 是一种选择性，具有口服活性的且具有 ATP 竞争性的 ALK 酪氨酸激酶抑制剂，IC₅₀ 为 200 pM。 Ceritinib (LDK378) 还抑制 IGF-1R，InsR 和 STK22D，IC₅₀ 值分别为 8、7 和 23 nM。Ceritinib (LDK378) 显示出良好抗肿瘤效力。

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Ceritinib Chemical Structure

CAS No. : 1032900-25-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥675	In-stock
5 mg	￥550	In-stock
10 mg	￥770	In-stock
50 mg	￥1100	In-stock
100 mg	￥1650	In-stock
200 mg	￥2640	In-stock
500 mg	￥4950	In-stock
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Customer Review

Other Forms of Ceritinib:

MCE 顾客使用本产品发表的 30 篇科研文献

: Ceritinib purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):996-1006. [Abstract]; Dose-response and time course comparison of ALK inhibition by Crizotinib or Ceritinib.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC₅₀ of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC₅₀ values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency^[1]^[2].

IC₅₀ & Target

IC50: 0.2 nM (ALK), 7 nM (InsR), 8 nM (IGF-1R), 23 nM (STK22D), 60 nM (FLT3), 260 nM (FGFR2)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
786-0	IC₅₀	2.7 μM Compound: LDK378	Antiproliferative activity against human 786-0 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human 786-0 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
A-375	IC₅₀	1.043 μM Compound: LDK378	Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
A549	IC₅₀	> 1 μM Compound: Ceritinib	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: 30223120]
A549	IC₅₀	> 1 μM Compound: Ceritinib	Antiproliferative activity against human A549 cells harboring EGFR after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring EGFR after 72 hrs by MTT assay	[PMID: 29174809]
A549	IC₅₀	> 10 μM Compound: Ceritinib	Antiproliferative activity against EGFR-positive human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against EGFR-positive human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34534734]
A549	IC₅₀	> 10 μM Compound: Ceritinib	Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 33756437]
A549	IC₅₀	> 10 μM Compound: Ceritinib	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hr by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hr by MTT assay	[PMID: 33069079]
A549	IC₅₀	> 10 μM Compound: LDK378	Cytotoxicity against EGFR-positive human A549 cells incubated for 72 hrs by MTT assay Cytotoxicity against EGFR-positive human A549 cells incubated for 72 hrs by MTT assay	[PMID: 33069075]
A549	IC₅₀	> 10 μM Compound: Ceritinib	Cytotoxicity against human A549 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay	[PMID: 27474925]
A549	IC₅₀	> 10 μM Compound: Ceritinib	Antiproliferative activity against human A549 cells by MTT assay Antiproliferative activity against human A549 cells by MTT assay	[PMID: 36113668]
A549	IC₅₀	0.081 μM Compound: Ceritinib	Cytotoxicity against human A549 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay	[PMID: 30927566]
A549	IC₅₀	0.51 μM Compound: Ceritinib	Antiproliferative activity against human A549 cells harbouring EGFR G1202R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells harbouring EGFR G1202R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31492532]
A549	IC₅₀	1.2 μM Compound: 2	Antiproliferative activity against ALK-negative human A549 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against ALK-negative human A549 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 35576654]
A549	IC₅₀	1.32 μM Compound: LDK378	Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33453602]
A549	IC₅₀	1.43 μM Compound: Ceritinib	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31492532]
A549	IC₅₀	1.61 μM Compound: Ceritinib	Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 33581554]
A549	IC₅₀	1.61 μM Compound: Ceritinib	Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 30927566]
A549	IC₅₀	2.142 μM Compound: LDK378	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
A549	IC₅₀	2.16 μM Compound: Ceritinib	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34237620]
A549	IC₅₀	2.72 μM Compound: Ceritinib	Antiproliferative activity against EGFR positive human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against EGFR positive human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
A549	IC₅₀	2.77 μM Compound: LDK378	Antiproliferative activity against EGFR-positive human A549 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against EGFR-positive human A549 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
A549	GI₅₀	845 nM Compound: 1	Cytotoxicity against ALK-negative human A549 cells harboring wild type PI3KCA and CDKN2A and KRAS mutations assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against ALK-negative human A549 cells harboring wild type PI3KCA and CDKN2A and KRAS mutations assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32184963]
AGS	IC₅₀	2.24 μM Compound: LDK378	Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
BaF3	IC₅₀	> 1 μM Compound: Ceritinib	Antiproliferative activity IL3 dependent human Ba/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity IL3 dependent human Ba/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
BaF3	IC₅₀	> 1 μM Compound: Ceritinib	Antiproliferative activity against mouse BAF3 cells harboring G1202R mutation after 72 hrs by MTT assay Antiproliferative activity against mouse BAF3 cells harboring G1202R mutation after 72 hrs by MTT assay	[PMID: 30223120]
BaF3	IC₅₀	> 1000 nM Compound: 3	Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	IC₅₀	> 1000 nM Compound: 3	Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	EC₅₀	> 3000 nM Compound: Ceritinib	Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	> 5 μM Compound: Ceritinib	Cytotoxicity against mouse BA/F3 cells incubated for 72 hrs by MTT assay Cytotoxicity against mouse BA/F3 cells incubated for 72 hrs by MTT assay	[PMID: 30927566]
BaF3	EC₅₀	> 5000 nM Compound: Ceritinib	Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	1.01 μM Compound: Ceritinib	Cytotoxicity against mouse BA/F3 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay Cytotoxicity against mouse BA/F3 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay	[PMID: 30927566]
BaF3	IC₅₀	10.7 nM Compound: 3	Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	IC₅₀	101 nM Compound: 2	Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	164 nM Compound: 2	Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	234 nM Compound: 3	Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	IC₅₀	2477 nM Compound: 2; LDK378	Antiproliferative activity against wild type mouse BaF3 cells assessed as reduction in cell growth incubated for 2 to 3 days by Bright-Glo luciferase assay Antiproliferative activity against wild type mouse BaF3 cells assessed as reduction in cell growth incubated for 2 to 3 days by Bright-Glo luciferase assay	[PMID: 26750252]
BaF3	IC₅₀	2477 nM Compound: 15b, LDK378	Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
BaF3	EC₅₀	2500 nM Compound: Ceritinib	Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	2500 nM Compound: Ceritinib	Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	26 nM Compound: Ceritinib	Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	26 nM Compound: 15b, LDK378	Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
BaF3	EC₅₀	2660 nM Compound: Ceritinib	Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	2747 nM Compound: 2	Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	EC₅₀	3000 nM Compound: Ceritinib	Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	319.5 nM Compound: 15b, LDK378	Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
BaF3	IC₅₀	33 nM Compound: 2	Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	41 nM Compound: 2	Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	444 nM Compound: 2	Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	54.9 nM Compound: 3	Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	IC₅₀	5512 nM Compound: 2	Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	57 nM Compound: 2	Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	576.6 nM Compound: 19	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	64 nM Compound: 2	Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	668 nM Compound: 2	Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	7.11 nM Compound: Ceritinib	Antiproliferative activity against mouse BaF3 cells overexpressing ALK assessed as inhibition of cell proliferation measured by CCK8 assay Antiproliferative activity against mouse BaF3 cells overexpressing ALK assessed as inhibition of cell proliferation measured by CCK8 assay	[PMID: 34245852]
BaF3	IC₅₀	726 nM Compound: 3	Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	CC₅₀	75 nM Compound: LDK378	Inhibition of ALK L1196M mutant in mouse BA/F3 cells assessed as inhibition of cell proliferation after 72 hrs by WST1 assay Inhibition of ALK L1196M mutant in mouse BA/F3 cells assessed as inhibition of cell proliferation after 72 hrs by WST1 assay	[PMID: 26923695]
BaF3	IC₅₀	780.5 nM Compound: 19	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
EA.hy 926	IC₅₀	1.01 μM Compound: Ceritinib	Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
HCC78	IC₅₀	> 1000 nM Compound: 3	Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
HCC78	IC₅₀	0.018 μM Compound: Ceritinib	Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay	[PMID: 27474925]
HCC78	IC₅₀	0.039 μM Compound: Ceritinib	Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31492532]
HCC78	IC₅₀	0.058 μM Compound: LDK378	Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 incubated for 72 hrs by MTT assay Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 incubated for 72 hrs by MTT assay	[PMID: 33069075]
HCC78	IC₅₀	0.058 μM Compound: Ceritinib	Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay	[PMID: 30223120]
HCC78	IC₅₀	0.058 μM Compound: Ceritinib	Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay	[PMID: 29174809]
HCC78	IC₅₀	0.067 μM Compound: Ceritinib	Cytotoxicity against human HCC78 cells incubated for 72 hrs by MTT assay Cytotoxicity against human HCC78 cells incubated for 72 hrs by MTT assay	[PMID: 30927566]
HCT-116	IC₅₀	1.07 μM Compound: 2	Antiproliferative activity against ALK-negative human HCT-116 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against ALK-negative human HCT-116 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 35576654]
HCT-116	IC₅₀	1.82 μM Compound: Ceritinib	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
HCT-116	IC₅₀	1.93 μM Compound: LDK378	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
HEK-293T	IC₅₀	> 10 μM Compound: Ceritinib	Antiproliferative activity against human HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
HeLa	IC₅₀	0.94 μM Compound: LDK378	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33453602]
Hep 3B2	IC₅₀	2.16 μM Compound: Ceritinib	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
HEp-2	IC₅₀	1.83 μM Compound: LDK378	Antiproliferative activity against human Hep2 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human Hep2 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
HepG2	IC₅₀	0.77 μM Compound: LDK378	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
HepG2	IC₅₀	4.08 μM Compound: Ceritinib	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34237620]
HK-2	IC₅₀	2.512 μM Compound: Ceritinib	Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
HT-29	IC₅₀	> 10 μM Compound: Ceritinib	Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay	[PMID: 27474925]
HT-29	IC₅₀	0.7 μM Compound: LDK378	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
HT-29	IC₅₀	1.03 μM Compound: Ceritinib	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31492532]
HT-29	IC₅₀	1.12 μM Compound: Ceritinib	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
Jurkat	IC₅₀	2.918 μM Compound: LDK378	Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
KARPAS-299	IC₅₀	0.013 μM Compound: LDK378	Antiproliferative activity against human KARPAS299 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human KARPAS299 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
KARPAS-299	IC₅₀	0.02 μM Compound: 2	Antiproliferative activity against NPM-ALK positive human KARPAS-299 cells assessed as inhibition of cell growth incubated for 96 hrs by CCK-8 assay Antiproliferative activity against NPM-ALK positive human KARPAS-299 cells assessed as inhibition of cell growth incubated for 96 hrs by CCK-8 assay	[PMID: 35576654]
KARPAS-299	IC₅₀	0.02 μM Compound: Ceritinib	Cytotoxicity against human KARPAS299 cells incubated for 72 hrs by MTT assay Cytotoxicity against human KARPAS299 cells incubated for 72 hrs by MTT assay	[PMID: 30927566]
KARPAS-299	IC₅₀	0.024 μM Compound: LDK378	Antiproliferative activity against NPM-ALK-positive human KARPAS-299 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against NPM-ALK-positive human KARPAS-299 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
KARPAS-299	IC₅₀	0.026 μM Compound: LDK378	Cytotoxicity against human KARPAS299 cells harboring NMP-ALK incubated for 72 hrs by MTT assay Cytotoxicity against human KARPAS299 cells harboring NMP-ALK incubated for 72 hrs by MTT assay	[PMID: 33069075]
KARPAS-299	IC₅₀	0.026 μM Compound: Ceritinib	Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay	[PMID: 29174809]
KARPAS-299	IC₅₀	0.027 μM Compound: Ceritinib	Antiproliferative activity against NPM-ALK positive human KARPAS-299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against NPM-ALK positive human KARPAS-299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
KARPAS-299	IC₅₀	0.027 μM Compound: Ceritinib	Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay	[PMID: 27474925]
KARPAS-299	IC₅₀	0.031 μM Compound: Ceritinib	Antiproliferative activity against human KARPAS-299 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human KARPAS-299 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 33756437]
KARPAS-299	IC₅₀	0.037 μM Compound: Ceritinib	Antiproliferative activity against human KARPAS299 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human KARPAS299 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31492532]
KARPAS-299	IC₅₀	0.041 μM Compound: Ceritinib	Antiproliferative activity against human Karpas299 cells assessed as reduction in cell viability incubated for 4 hr by MTT assay Antiproliferative activity against human Karpas299 cells assessed as reduction in cell viability incubated for 4 hr by MTT assay	[PMID: 33069079]
KARPAS-299	IC₅₀	0.041 μM Compound: Ceritinib	Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay	[PMID: 30223120]
KARPAS-299	IC₅₀	0.042 μM Compound: Ceritinib	Antiproliferative activity against NPM-ALK addicted human KARPAS-299 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against NPM-ALK addicted human KARPAS-299 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34534734]
KARPAS-299	IC₅₀	0.047 μM Compound: Ceritinib	Antiproliferative activity against human KARPAS-299 cells by MTT assay Antiproliferative activity against human KARPAS-299 cells by MTT assay	[PMID: 36113668]
KARPAS-299	IC₅₀	0.08 μM Compound: Ceritinib	Antiproliferative activity against human KARPAS-299 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human KARPAS-299 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 33581554]
KARPAS-299	IC₅₀	22.8 nM Compound: 15b, LDK378	Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
KARPAS-299	IC₅₀	84 nM Compound: 3	Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
Kelly	EC₅₀	142 nM Compound: 2	Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
KM12	IC₅₀	0.728 μM Compound: Ceritinib	Antiproliferative activity against TPM3-NTRK1-addicted human KM12 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against TPM3-NTRK1-addicted human KM12 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34534734]
MCF7	IC₅₀	> 10 μM Compound: Ceritinib	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: 33581554]
MCF7	IC₅₀	1.65 μM Compound: Ceritinib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
MCF7	IC₅₀	1.754 μM Compound: LDK378	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
MCF7	IC₅₀	1.87 μM Compound: LDK378	Antiproliferative activity against human MCF7 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
MDA-MB-231	IC₅₀	1.82 μM Compound: Ceritinib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34237620]
MDA-MB-231	IC₅₀	2.71 μM Compound: Ceritinib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
MDA-MB-468	IC₅₀	2.708 μM Compound: LDK378	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
NCI-H1299	IC₅₀	2.92 μM Compound: LDK378	Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33453602]
NCI-H1581	IC₅₀	2.18 μM Compound: Ceritinib	Antiproliferative activity against human NC-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NC-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
NCI-H1581	IC₅₀	2.31 μM Compound: LDK378	Antiproliferative activity against human NCI-H1581 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human NCI-H1581 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H1975	IC₅₀	> 10 μM Compound: LDK378	Cytotoxicity against EGFR-positive human H1975 cells incubated for 72 hrs by MTT assay Cytotoxicity against EGFR-positive human H1975 cells incubated for 72 hrs by MTT assay	[PMID: 33069075]
NCI-H2228	CC₅₀	0.025 μM Compound: LDK378	Cytotoxicity against human NCI-H2228 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay Cytotoxicity against human NCI-H2228 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay	[PMID: 26712094]
NCI-H2228	IC₅₀	0.026 μM Compound: Ceritinib	Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay	[PMID: 30223120]
NCI-H2228	IC₅₀	0.03 μM Compound: 2	Antiproliferative activity against EML4-ALK positive human NCI-H2228 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against EML4-ALK positive human NCI-H2228 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 35576654]
NCI-H2228	IC₅₀	0.045 μM Compound: Ceritinib	Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31492532]
NCI-H2228	IC₅₀	0.066 μM Compound: LDK378	Antiproliferative activity against EML4-ALK-positive human NCI-H2228 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against EML4-ALK-positive human NCI-H2228 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H2228	IC₅₀	0.079 μM Compound: Ceritinib	Antiproliferative activity against EML4-ALK positive human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against EML4-ALK positive human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
NCI-H2228	IC₅₀	0.099 μM Compound: Ceritinib	Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay	[PMID: 29174809]
NCI-H2228	IC₅₀	0.104 μM Compound: Ceritinib	Antiproliferative activity against EML4-ALK addicted human H2228 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against EML4-ALK addicted human H2228 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34534734]
NCI-H2228	IC₅₀	0.107 μM Compound: Ceritinib	Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 33756437]
NCI-H2228	IC₅₀	0.15 μM Compound: Ceritinib	Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 33581554]
NCI-H2228	IC₅₀	0.15 μM Compound: Ceritinib	Cytotoxicity against human NCI-H2228 cells incubated for 72 hrs by MTT assay Cytotoxicity against human NCI-H2228 cells incubated for 72 hrs by MTT assay	[PMID: 30927566]
NCI-H2228	IC₅₀	0.162 μM Compound: Ceritinib	Antiproliferative activity against human NCI-H2228 cells by MTT assay Antiproliferative activity against human NCI-H2228 cells by MTT assay	[PMID: 36113668]
NCI-H2228	IC₅₀	1.07 μM Compound: Ceritinib	Antiproliferative activity against human H2228 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human H2228 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33069079]
NCI-H2228	IC₅₀	1.3 μM Compound: LDK378	Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33453602]
NCI-H2228	IC₅₀	1.98 μM Compound: Ceritinib	Antiproliferative activity against human NCI-H2228 cells harboring EML4/ALK L1196M mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H2228 cells harboring EML4/ALK L1196M mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34237620]
NCI-H2228	IC₅₀	102.6 nM Compound: Ceritinib	Cytotoxicity against human NCI-H2228 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against human NCI-H2228 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 25644671]
NCI-H2228	IC₅₀	15 nM Compound: 2	Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay	[PMID: 29627725]
NCI-H2228	IC₅₀	2.9 μM Compound: LDK378	Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay	[PMID: 31425908]
NCI-H2228	IC₅₀	22.1 nM Compound: Ceritinib	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell proliferation measured by CCK8 assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell proliferation measured by CCK8 assay	[PMID: 34245852]
NCI-H3122	IC₅₀	0.018 μM Compound: LDK378	Antiproliferative activity against human NCI-H3122 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human NCI-H3122 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
NCI-H3122	CC₅₀	0.038 μM Compound: LDK378	Cytotoxicity against human NCI-H3122 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay Cytotoxicity against human NCI-H3122 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay	[PMID: 26712094]
NCI-H3122	IC₅₀	0.043 μM Compound: LDK378	Antiproliferative activity against EML4-ALK-positive human NCI-H3122 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against EML4-ALK-positive human NCI-H3122 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H3122	IC₅₀	0.043 μM Compound: Ceritinib	Antiproliferative activity against EML4-ALK positive human NC-H3122 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against EML4-ALK positive human NC-H3122 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
NCI-H3122	IC₅₀	1.1 μM Compound: Ceritinib	Antiproliferative activity against human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33471528]
NCI-H3122	IC₅₀	1.1 μM Compound: LDK378	Antiproliferative activity against human NCI-H3122 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33453602]
NCI-H3122	EC₅₀	15 nM Compound: 2	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
NCI-H3122	IC₅₀	96 nM Compound: 3	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
NCI-H460	IC₅₀	> 1 μM Compound: Ceritinib	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: 29174809]
NCI-H460	IC₅₀	> 10 μM Compound: Ceritinib	Cytotoxicity against human NCI-H460 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay Cytotoxicity against human NCI-H460 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay	[PMID: 27474925]
NCI-H460	IC₅₀	10.32 μM Compound: LDK378	Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
PC-3	IC₅₀	0.76 μM Compound: LDK378	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
PC-3	IC₅₀	0.941 μM Compound: Ceritinib	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
PC-3	IC₅₀	1.02 μM Compound: LDK378	Antiproliferative activity against human PC-3 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human PC-3 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
Raji	IC₅₀	0.49 μM Compound: LDK378	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
SH-SY5Y	IC₅₀	0.37 μM Compound: Ceritinib	Antiproliferative activity against human SH-SY5Y cells harboring ALK F1174L mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human SH-SY5Y cells harboring ALK F1174L mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34237620]
SH-SY5Y	EC₅₀	186 nM Compound: 2	Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-AS	EC₅₀	1045 nM Compound: 2	Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-FI	EC₅₀	349 nM Compound: 2	Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-SH	EC₅₀	303 nM Compound: 2	Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SU-DHL-1	IC₅₀	122 nM Compound: 3	Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
SU-DHL-1	IC₅₀	15 nM Compound: 2	Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay	[PMID: 29627725]
U2OS	IC₅₀	0.85 μM Compound: LDK378	Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 31177074]
Vero	IC₅₀	2.86 μM Compound: LDK378	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730
Vero	CC₅₀	6.84 μM Compound: LDK378	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730

体外研究
(In Vitro)

Ceritinib (LDK378) 还抑制 RET (IC₅₀=400 nM)、FGFR3 (IC₅₀=430 nM)、LCK (IC₅₀= 560 nM)，JAK2 (IC₅₀=610 nM)，Aurora (IC₅₀=660 nM)，LYN (₅₀=840 nM)，EGFR (IC₅₀=900 nM)，FGFR4 (IC₅₀=950 nM)^[1]。
Ceritinib (LDK378) 对 ALK 酶活性保持高效力，IC₅₀ 值为 200 pM，并且仅对一组 46 种激酶中的 IGF-1R、InsR 和 STK22D 具有强抑制作用，具有最低选择性为 70 倍。在转染各种激酶的 Ba/F3 细胞中，Ceritinib 抑制 ALK 活性，IC₅₀ 值为 40.7 nM，IC₅₀ 值 >100 nM 对抗所有其他测试的激酶. Ceritinib (LDK378) 在携带 NPM-ALK 融合基因的 Karpas 299 人非霍奇金 K_i 阳性大细胞淋巴瘤中显示出有效的抗增殖活性，IC₅₀ 值为 22.8 nM基因和 26 nM 在转染了 NPM-ALK 融合基因的 Ba/F3 细胞中。Ceritinib 对野生型 Ba/F3 细胞 (IC₅₀>2 μM) 和转染 Tel-InsR 基因的 Ba/F3 细胞 (IC₅₀=320) 也表现出良好的选择性nM)^[2]。

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

体内研究
(In Vivo)

Ceritinib (LDK378) 在啮齿动物和非啮齿动物中具有出色的药代动力学特征，口服生物利用度 >50%。Ceritinib 在每日给药的 Karpas 299 大鼠异种移植模型中表现出剂量依赖性肿瘤生长抑制并实现部分肿瘤消退，但能够在携带 EML4-ALK 融合基因的 H2228 NSCLC 大鼠异种移植模型中实现完全肿瘤消退。在这两种模型中，Ceritinib (LDK378) 在动物中的耐受性良好。Ceritinib (LDK378) 的 ADME 谱得到进一步评估，发现其在肝微粒体中具有相对良好的代谢稳定性、适度的 CYP3A4 抑制和一些 hERG 抑制，在 hERG 贴片中的 IC₅₀ 值为 46 μM夹实验，但在狗和猴子遥测研究中都没有 QTc 延长的证据^[2]。

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

Clinical Trial

分子量

558.14

Formula

C₂₈H₃₆ClN₅O₃S

CAS 号

1032900-25-6

性状

固体

颜色

White to off-white

中文名称

色瑞替尼

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 : 12.5 mg/mL (22.40 mM; 超声助溶 (<60°C); 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	1.7917 mL	8.9583 mL	17.9167 mL
5 mM	0.3583 mL	1.7917 mL	3.5833 mL
10 mM	0.1792 mL	0.8958 mL	1.7917 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： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (0.90 mM); 澄清溶液

此方案可获得 ≥ 0.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 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。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (0.90 mM); 澄清溶液

此方案可获得 ≥ 0.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 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。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 0.5 mg/mL (0.90 mM); 澄清溶液

此方案可获得 ≥ 0.5 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 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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: 99.98%

选择批次：

Data Sheet (653 KB) SDS (393 KB)

COA (287 KB) RP-HPLC (206 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Marsilje TH, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25;56(14):5675-90. [Content Brief]

[2]. Chen J, et al. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56(14):5673-4. [Content Brief]

[3]. Tucker ER, et al. Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. Mol Oncol. 2017 Aug;11(8):996-1006. [Content Brief]

[4]. Rothschild SI. Ceritinib-a second-generation ALK inhibitor overcoming resistance in ALK-rearranged non-small celllung cancer. Transl Lung Cancer Res. 2014 Dec;3(6):379-81. [Content Brief]

Animal Administration ^[1]	In vivo PK studies are conducted in mice, rats, dogs, and cynomolgus monkeys. Ceritinib (LDK378) (HCl salt) is administered to male Balb/c mice intravenously via tail vein at 5 mg/kg (n=3) and orally via gavage at 20 mg/kg (n=3). By use of the same formulation, Ceritinib (LDK378) (HCl salt) is dosed to Sprague-Dawley rats intravenously via the tail vein at 3 mg/kg (n=3) and orally via gavage at 10 mg/kg (n=3). Blood samples are collected serially at scheduled times over 24 h after dosing. Male beagle dogs receive a single intravenous (n=2) or oral (n=3) dose of Ceritinib (phosphate salt) as an intravenous solution at 5 mg/kg and an oral suspension at 20 mg/kg, respectively. Male cynomologus monkeys receive single intravenous (n=2) or oral (n=3) dose of Ceritinib (free base) as an intravenous solution at 5 mg/kg and an oral suspension at 60 mg/kg, respectively. Blood samples for plasma are collected at prescheduled times over 144 h after dosing^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Marsilje TH, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25;56(14):5675-90. [Content Brief] [2]. Chen J, et al. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56(14):5673-4. [Content Brief] [3]. Tucker ER, et al. Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. Mol Oncol. 2017 Aug;11(8):996-1006. [Content Brief] [4]. Rothschild SI. Ceritinib-a second-generation ALK inhibitor overcoming resistance in ALK-rearranged non-small celllung cancer. Transl Lung Cancer Res. 2014 Dec;3(6):379-81. [Content Brief]

Animal Administration
^[1]

In vivo PK studies are conducted in mice, rats, dogs, and cynomolgus monkeys. Ceritinib (LDK378) (HCl salt) is administered to male Balb/c mice intravenously via tail vein at 5 mg/kg (n=3) and orally via gavage at 20 mg/kg (n=3). By use of the same formulation, Ceritinib (LDK378) (HCl salt) is dosed to Sprague-Dawley rats intravenously via the tail vein at 3 mg/kg (n=3) and orally via gavage at 10 mg/kg (n=3). Blood samples are collected serially at scheduled times over 24 h after dosing. Male beagle dogs receive a single intravenous (n=2) or oral (n=3) dose of Ceritinib (phosphate salt) as an intravenous solution at 5 mg/kg and an oral suspension at 20 mg/kg, respectively. Male cynomologus monkeys receive single intravenous (n=2) or oral (n=3) dose of Ceritinib (free base) as an intravenous solution at 5 mg/kg and an oral suspension at 60 mg/kg, respectively. Blood samples for plasma are collected at prescheduled times over 144 h after dosing^[1].

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

参考文献

[1]. Marsilje TH, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25;56(14):5675-90. [Content Brief]

[2]. Chen J, et al. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56(14):5673-4. [Content Brief]

[3]. Tucker ER, et al. Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. Mol Oncol. 2017 Aug;11(8):996-1006. [Content Brief]

[4]. Rothschild SI. Ceritinib-a second-generation ALK inhibitor overcoming resistance in ALK-rearranged non-small celllung cancer. Transl Lung Cancer Res. 2014 Dec;3(6):379-81. [Content Brief]

Ceritinib 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	1.7917 mL	8.9583 mL	17.9167 mL	44.7916 mL
	5 mM	0.3583 mL	1.7917 mL	3.5833 mL	8.9583 mL
	10 mM	0.1792 mL	0.8958 mL	1.7917 mL	4.4792 mL
	15 mM	0.1194 mL	0.5972 mL	1.1944 mL	2.9861 mL
	20 mM	0.0896 mL	0.4479 mL	0.8958 mL	2.2396 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:

Ceritinib1032900-25-6LDK378色瑞替尼LDK 378LDK-378Anaplastic lymphoma kinase (ALK)Insulin ReceptorIGF-1RAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Insulin-like growth factor-1 receptorInhibitorinhibitorinhibit

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Ceritinib (Synonyms: 色瑞替尼; LDK378)

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Ceritinib (Synonyms: 色瑞替尼; LDK378)

Customer Review

Other Forms of Ceritinib:

Ceritinib 相关抗体

MCE 顾客使用本产品发表的 30 篇科研文献

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