製品番号: HY-15656

Ceritinib

(別名: LDK378)

43 Cited Publications

カスタマーレビュー

Based on 43 publication(s) in Google Scholar

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

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純度: 99.95%
CAS 番号: 1032900-25-6
分子式: C₂₈H₃₆ClN₅O₃S
分子量:558.14

保管条件:

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

Ceritinib 構造式

CAS 番号: 1032900-25-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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製品説明

IC₅₀ & Target

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

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	>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	>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	>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	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	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	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	1.43 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	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]
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	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	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	1.61 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	>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	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	>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	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	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	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]
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	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	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	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	>2 μM Compound: 6, LDK378	Cytotoxicity against wild type mouse BA/F3 cells assessed as growth inhibition Cytotoxicity against wild type mouse BA/F3 cells assessed as growth inhibition	[PMID: 23837797]
BaF3	IC₅₀	26 nM Compound: 6, LDK378	Cytotoxicity against mouse BA/F3 cells expressing NPM-ALK fusion gene assessed as growth inhibition Cytotoxicity against mouse BA/F3 cells expressing NPM-ALK fusion gene assessed as growth inhibition	[PMID: 23837797]
BaF3	IC₅₀	320 nM Compound: 6, LDK378	Cytotoxicity against mouse BA/F3 cells transfected with Tel-InsR gene assessed as growth inhibition Cytotoxicity against mouse BA/F3 cells transfected with Tel-InsR gene assessed as growth inhibition	[PMID: 23837797]
BaF3	IC₅₀	40.7 nM Compound: 6, LDK378	Inhibition of ALK (unknown origin) transfected in mouse BA/F3 cells Inhibition of ALK (unknown origin) transfected in mouse BA/F3 cells	[PMID: 23837797]
BaF3	IC₅₀	>2000 nM Compound: LDK378	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	44 nM Compound: LDK378	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	60 nM Compound: LDK378	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	CC₅₀	75 nM Compound: LDK378	Antiproliferative activity against mouse BAF3 cells expressing ALK L1196M mutant Antiproliferative activity against mouse BAF3 cells expressing ALK L1196M mutant	[PMID: 26235945]
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	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	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	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	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	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	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	1666 nM Compound: Ceritinib	Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth in presence of IL-3 Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth in presence of IL-3	[PMID: 27780853]
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	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	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	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	EC₅₀	3 μM 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	>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	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	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	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	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	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	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	>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	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	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	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]
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	>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]
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	226 nM Compound: LDK378	Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
HCC78	IC₅₀	506 nM Compound: LDK378	Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
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	0.058 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	>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	0.058 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	0.067 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]
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]
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	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	22.8 nM Compound: 6, LDK378	Cytotoxicity against human KARPAS299 cells expressing NPM-ALK fusion gene assessed as growth inhibition Cytotoxicity against human KARPAS299 cells expressing NPM-ALK fusion gene assessed as growth inhibition	[PMID: 23837797]
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	0.026 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	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]
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	0.02 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	0.013 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	0.037 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	0.026 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	0.041 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	0.08 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	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	0.042 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	0.02 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	0.027 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	0.024 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	0.047 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]
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]
L02	IC₅₀	1.03 μM Compound: Cer	Cytotoxicity against human L02 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
L02	IC₅₀	3.51 μM Compound: Cer	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
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	>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	1.87 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-H1299	IC₅₀	1.62 μM Compound: Cer	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H1299	IC₅₀	1.74 μM Compound: Cer	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
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	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	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	0.099 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	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	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	0.15 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	97 nM Compound: 16; LDK378	Growth inhibition of human NCI-H2228 cells Growth inhibition of human NCI-H2228 cells	[PMID: 31005443]
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	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	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	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	0.107 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	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	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-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	0.03 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	0.079 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	0.066 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	0.162 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	0.58 μM Compound: Cer	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H2228	IC₅₀	0.59 μM Compound: Cer	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H3122	CC₅₀	38 nM Compound: LDK378	Antiproliferative activity against wild type human NCI-H3122 cells Antiproliferative activity against wild type human NCI-H3122 cells	[PMID: 26235945]
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	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	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-H3122	IC₅₀	27.2 nM Compound: 16; LDK378	Growth inhibition of human NCI-H3122 cells Growth inhibition of human NCI-H3122 cells	[PMID: 31005443]
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	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	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	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	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	0.06 μM Compound: Cer	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H3122	IC₅₀	0.06 μM Compound: Cer	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
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	>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	10.32 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	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]
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]
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]
SR	IC₅₀	2.2 nM Compound: Ceritinib	Antiproliferative activity against ALK positive human SR cells Antiproliferative activity against ALK positive human SR cells	[PMID: 33751979]
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	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
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

体外実験

Ceritinib also inhibits 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), and FGFR4 (IC₅₀=950 nM)^[1].
Ceritinib retains high potency against the ALK enzymatic activity with an IC₅₀ value of 200 pM and shows only strong inhibition against IGF-1R, InsR, and STK22D out of a panel of 46 kinases with a minimum selectivity of 70-fold. In Ba/F3 cells transfected with various kinases, Ceritinib inhibits ALK activity with an IC₅₀ value of 40.7 nM and had IC₅₀ values of >100 nM against all other kinases tested. Ceritinib (LDK378) shows potent antiproliferative activity with an IC₅₀ value of 22.8 nM in Karpas 299 human non-Hodgkin’s K_i-positive large cell lymphoma carrying the NPM-ALK fusion gene and 26 nM in Ba/F3 cells transfected with the NPM-ALK fusion gene. Ceritinib also shows good selectivity over wild-type Ba/F3 cells (IC₅₀>2 μM) and Ba/F3 cells transfected with Tel-InsR gene (IC₅₀=320 nM)^[2].

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

体内実験

Ceritinib has an excellent pharmacokinetics profile in rodents and non-rodents with an oral bioavailability of >50%. Ceritinib demonstrates dose-dependent tumor growth inhibition and achieved partial tumor regression in the Karpas 299 rat xenograft model with daily administration but is capable of achieving complete tumor regression in the H2228 NSCLC rat xenograft model, which carries the EML4-ALK fusion gene. In both models, Ceritinib is well tolerated in animals. Ceritinib is further assessed for its ADME profile and is found to have a relatively good metabolic stability in liver microsomes, modest CYP3A4 inhibition, some hERG inhibition with an IC₅₀ value of 46 μM in hERG patch clamp experiments, but no evidence of QTc prolongation in both dog and monkey telemetry studies^[2].

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1032900-25-6
性状 Solid
分子量 558.14
分子式 C₂₈H₃₆ClN₅O₃S
Color White to off-white
SMILES

CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3
別名

LDK378
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (43)

All Cell Imaging/StainingIn Vivo Efficacy StudyWBCell Proliferation/Viability Assay

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Nat Cancer

Targeting the ALK-CDK9-Tyr19 kinase cascade sensitizes ovarian and breast tumors to PARP inhibition via destabilization of the P-TEFb complex. [Abstract]

2022 Oct;3(10):1211-1227. PMID: 36253486

Ceritinib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]

Oral olaparib (50 mg/kg) and ceritinib (7.5 mg/kg), either alone or in combination, five times per week, Tumor volume and Kaplan–Meier survival curves of mice bearing subcutaneous injected SKOV3 ovarian tumors.

Ceritinib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]

Western blot analysis of indicated proteins in PARPi-sensitive triple-negative breast cancer (TNBC) cells (parental) and TNBC cells with acquired resistance to PARPi (#6 and #15) treated with 50 nM PARPi (talazoparib) or 0.5 µM ALK inhibitor (ALKi; ceritinib), either alone or in combination, for 48 hours.

Ceritinib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]

Representative images of clonogenic assay results in PARPiresistant ovarian and TNBC cells in the presence of the indicated inhibitor for 12 days. Synergistic inhibition of cell proliferation is defined as CI < 1. CER, ceritinib; OLA, olaparib; Comb, combination of ceritinib and olaparib.
Nat Commun

Molecular landscape, subtypes, and therapeutic vulnerabilities of central nervous system solitary fibrous tumors. [Abstract]

2025 Aug 23;16(1):7870. PMID: 40849425
Nat Commun

Targeting NRAS via miR-1304-5p or farnesyltransferase inhibition confers sensitivity to ALK inhibitors in ALK-mutant neuroblastoma. [Abstract]

2024 Apr 23;15(1):3422. PMID: 38653965

Ceritinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Apr 23;15(1):3422. [Abstract]

At 48 h following transfection, the cells were treated with increasing concentrations of ceritinib for 72 h.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Discov

Phase separation of EML4-ALK in firing downstream signaling and promoting lung tumorigenesis. [Abstract]

2021 May 11;7(1):33. PMID: 33976114

Ceritinib purchased from MedChemExpress. Usage Cited in: Cell Discov. 2021 May 11;7(1):33. [Abstract]

BEAS-2B cells were transfected with GFP–EML4–ALK for 24 h. Cells were treated with DMSO or ALK inhibitors, alectinib (500 nM), ceritinib (500 nM), and GFP fluorescence was monitored through live imaging for up to 12 h.
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Cell Rep Med

Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]

2023 Feb 21;4(2):100911. PMID: 36657446
Pharmacol Res

Ceritinib inhibits growth and ACTH production of PitNETs: Insights from patient-derived organoids. [Abstract]

2025 Nov:221:107993. PMID: 41083089
Cancer Lett

Integrated clinical, genomic and functional characterization of a novel ALK variant in neuroblastoma. [Abstract]

2026 May 29:656:218624. PMID: 42217560
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
J Transl Med

Pulmonary midkine inhibition ameliorates sepsis induced lung injury. [Abstract]

2021 Feb 27;19(1):91. PMID: 33639987
Cell Chem Biol

Overcoming Resistance to Targeted Anticancer Therapies through Small-Molecule-Mediated MEK Degradation. [Abstract]

2018 Aug 16;25(8):996-1005.e4. PMID: 29909991
J Med Chem

Discovery of Oral Degraders of the ROS1 Fusion Protein with Potent Activity against Secondary Resistance Mutations. [Abstract]

2024 Oct 24;67(20):18098-18123. PMID: 39361251
Sci Signal

Pleiotrophin promotes vascular abnormalization in gliomas and correlates with poor survival in patients with astrocytomas. [Abstract]

2015 Dec 8;8(406):ra125. PMID: 26645582
Eur J Med Chem

Pyrimidine derivatives with antitubercular activity. [Abstract]

2023 Jan 15:246:114946. PMID: 36459759
Pharmaceuticals (Basel)

Therapeutic Implications of Ceritinib in Cholangiocarcinoma beyond ALK Expression and Mutation. [Abstract]

2024 Feb 2;17(2):197. PMID: 38399413
RSC Adv

Development and validation of an UPLC-ESI-MS/MS method for quantification of duvelisib in plasma: application to pharmacokinetic study in rats. [Abstract]

2023 Mar 10;13(12):7929-7938. PMID: 36909770
Mol Oncol

Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. [Abstract]

2017 Aug;11(8):996-1006. PMID: 28432815

Ceritinib purchased from MedChemExpress. 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.
iScience

Ceritinib induces ferroptosis via TRIM21-mediated GLUT1 ubiquitination and AMPK-driven metabolic reprogramming in breast cancer. [Abstract]

2026 Apr 22;29(6):115846. PMID: 42181273
Antiviral Res

Repurposing screen using a robust human rhinovirus infectious clone identifies pyrvinium pamoate with antiviral activity. [Abstract]

2026 Jun:250:106417. PMID: 42025967
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
AMB Express

Insights into the antimicrobial effects of ceritinib against Staphylococcus aureus in vitro and in vivo by cell membrane disruption. [Abstract]

2022 Nov 28;12(1):150. PMID: 36443539
Cell Signal

EML4-ALK G1202R mutation induces EMT and confers resistance to ceritinib in NSCLC cells via activation of STAT3/Slug signaling. [Abstract]

2022 Apr:92:110264. PMID: 35085771
Biochim Biophys Acta Mol Cell Res

ZX-29, a novel ALK inhibitor, induces apoptosis via ER stress in ALK rearrangement NSCLC cells and overcomes cell resistance caused by an ALK mutation. [Abstract]

2020 Jul;1867(7):118712. PMID: 32224191
Toxicol Appl Pharmacol

Ceritinib (LDK378) inhibits laryngeal squamous cell carcinoma progression via regulating ROS-induced mitochondrial apoptosis and inducing oxidative stress. [Abstract]

2025 Oct:503:117489. PMID: 40744212
Toxicol Appl Pharmacol

A novel ALK inhibitor ZYY inhibits Karpas299 cell growth in vitro and in a mouse xenograft model and induces protective autophagy. [Abstract]

2019 Nov 15;383:114781. PMID: 31618659
Analyst

Determination of veliparib metabolic stability in the human liver microsomes using a hydrophilic interaction UPLC-MS/MS quantitative method: greenness assessment with an in silico study for ADME, DEREK alarms and metabolic lability. [Abstract]

2025 Dec 1;150(24):5501-5513. PMID: 41231074
Anim Reprod Sci

Differential impact of the kinase inhibitors ruxolitinib and ceritinib on porcine sperm in vitro. [Abstract]

2025 Apr 28:277:107850. PMID: 40318512
J Pharm Pharmacol

1-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)-3-(2-(dimethylamino)ethyl)imidazolidin-2-one (ZX-42), a novel ALK inhibitor, induces apoptosis and protective autophagy in H2228 cells. [Abstract]

2020 Oct;72(10):1370-1382. PMID: 32596809
PLoS One

Inhibition of the anti-apoptotic protein BCL2 in EML4-ALK cell models as a second proposed therapeutic target for non-small cell lung cancer. [Abstract]

2025 Jan 21;20(1):e0308747. PMID: 39836700
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
Cancer Chemother Pharmacol

Targeting ALK in pediatric RMS does not induce antitumor activity in vivo. [Abstract]

2018 Aug;82(2):251-263. PMID: 29855693
Cell Physiol Biochem

Inhibition of Collagen Related Peptide Induced Platelet Activation and Apoptosis by Ceritinib. [Abstract]

2018;45(4):1707-1716. PMID: 29490295
Biol Methods Protoc

Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]

2025 Feb 13;10(1):bpaf012. PMID: 40060949
Xenobiotica

Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1. [Abstract]

2018 Oct;48(10):1059-1071. PMID: 29034773
bioRxiv

2023 Jul 19.
Patent

US20230158019A1.
Universitat Autònoma de Barcelona

2022 Aug.
Uppsala University

2022 Feb.
Patent

US20200276189A1.

溶剤 & 溶解度

体外:

DMSO : 12.5 mg/mL (22.40 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

モル濃度計算機

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分子量分子量

希釈計算機

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濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.5 mg/mL (0.90 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.5 mg/mL (0.90 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.5 mg/mL (0.90 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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%
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

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].

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (279 KB)
SDS (393 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
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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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	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

Keywords

Ceritinib

43 Cited Publications

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Ceritinib

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MedChemExpress（MCE）の使用を引用している文献 Ceritinib

生物活性

化学情報

Publications (43)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Ceritinib 関連分類

HY-15656 関連分類