Ceritinib (Synonyms: LDK378)

Name: Ceritinib
Brand: MedChemExpress
SKU: HY-15656
Rating: 5.0 (31 reviews)

Cat. No.: HY-15656 Purity: 99.98%: FAQs
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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.

For research use only. We do not sell to patients.

Ceritinib Chemical Structure

CAS No. : 1032900-25-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 67	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 67	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 31 publication(s) in Google Scholar

Other Forms of Ceritinib:

30 Publications Citing Use of MCE Ceritinib

: 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.

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Description

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	> 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

In Vitro

Ceritinib (LDK378) 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 (LDK378) 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.

In Vivo

Ceritinib (LDK378) 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 (LDK378) is well tolerated in animals. Ceritinib (LDK378) 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.

Clinical Trial

Molecular Weight

558.14

Formula

C₂₈H₃₆ClN₅O₃S

CAS No.

1032900-25-6

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (249 KB) RP-HPLC (206 KB)

Handling Instructions (2659 KB)

References

[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.

References

[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]

Complete Stock Solution Preparation Table

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

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

Keywords:

Ceritinib1032900-25-6LDK378LDK 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: LDK378)

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