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Ceritinib ALK inhibitor

Name: Ceritinib
Brand: Selleck Chemicals
SKU: S7083
Availability: InStock
Rating: 5 (118 reviews)

Cat.No.S7083

Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. This compound also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.

Chemical Structure

Molecular Weight: 558.14

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Other ALK Products	TAE684 (NVP-TAE684) GSK1838705A Repotrectinib (TPX-0005) AZD3463 AP26113-analog (ALK-IN-1) Ensartinib dihydrochloride ASP3026 HG-14-10-04 X-376 ALK inhibitor 1

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Parental(+IL3)	Growth Inhibition Assay		72 h	DMSO	IC50=1586 ± 173 nM	25749034
WT 70	Growth Inhibition Assay		72 h	DMSO	IC50=21 ± 8 nM	25749034
G1128S 1022	Growth Inhibition Assay		72 h	DMSO	IC50=102 ± 38 nM	25749034
C1156F 1293	Growth Inhibition Assay		72 h	DMSO	IC50=217 ± 115 nM	25749034
I1171N 519	Growth Inhibition Assay		72 h	DMSO	IC50=187 ± 87 nM	25749034
I1171T 445	Growth Inhibition Assay		72 h	DMSO	IC50=82 ± 12 nM	25749034
F1174I 184	Growth Inhibition Assay		72 h	DMSO	IC50=13 ± 0.1 nM	25749034
N1178H 169	Growth Inhibition Assay		72 h	DMSO	IC50=42 ± 6 nM	25749034
E1210K 748	Growth Inhibition Assay		72 h	DMSO	IC50=187 ± 84 nM	25749034
C1156F/D1203N 2809	Growth Inhibition Assay		72 h	DMSO	IC50=254 ± 99 nM	25749034
Ba/F3 NA WT	Growth Inhibition Assay		72 h		IC50=0.020 μM	25727400
Ba/F3 NA C1156Y	Growth Inhibition Assay		72 h		IC50=0.071 μM	25727400
Ba/F3 NA L1196M	Growth Inhibition Assay		72 h		IC50=0.042 μM	25727400
Ba/F3 NA L1152R	Growth Inhibition Assay		72 h		IC50=0.288 μM	25727400
Ba/F3 NA G1202R	Growth Inhibition Assay		72 h		IC50=0.277 μM	25727400
Ba/F3 NA G1269A	Growth Inhibition Assay		72 h		IC50=0.019 μM	25727400
Ba/F3 NA S1206Y	Growth Inhibition Assay		72 h		IC50=0.037 μM	25727400
Ba/F3 EA WT	Growth Inhibition Assay		72 h		IC50=0.021 μM	25727400
Ba/F3 EA C1156Y	Growth Inhibition Assay		72 h		IC50=0.026 μM	25727400
Ba/F3 EA L1196M	Growth Inhibition Assay		72 h		IC50=0.019 μM	25727400
Ba/F3 EA L1152R	Growth Inhibition Assay		72 h		IC50=0.099 μM	25727400
Ba/F3 EA G1202R	Growth Inhibition Assay		72 h		IC50=0.467 μM	25727400
Ba/F3 EA G1269A	Growth Inhibition Assay		72 h		IC50=0.033 μM	25727400
Ba/F3 EA S1206Y	Growth Inhibition Assay		72 h		IC50=0.038 μM	25727400
BAF3	Antiproliferative assay		72 hrs		Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.0107 μM.	29288940
NCI-H3122	Antiproliferative assay		72 hrs		Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.015 μM.	26568289
NCI-H2228	Growth inhibition assay		3 days		Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay, IC50 = 0.015 μM.	29627725
SU-DHL1	Growth inhibition assay		3 days		Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay, IC50 = 0.015 μM.	29627725
DFCI114	Antiproliferative assay		72 hrs		Antiproliferative activity against human DFCI114 cells expressing EML4-ALK G1269A mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.018 μM.	26568289
HCC78	Cytotoxicity assay		72 hrs		Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay, IC50 = 0.018 μM.	27474925
KARPAS299	Cytotoxicity assay		2 to 3 days		Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 0.0228 μM.	23742252
KARPAS299	Cytotoxicity assay				Cytotoxicity against human KARPAS299 cells expressing NPM-ALK fusion gene assessed as growth inhibition, IC50 = 0.0228 μM.	23837797
NCI-H3122	Function assay		72 hrs		Inhibition of EML4 fused ALK in human NCI-H3122 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay, CC50 = 0.025 μM.	27915169
BAF3	Function assay		2 to 3 days		Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 0.026 μM.	23742252
BA/F3	Cytotoxicity assay				Cytotoxicity against mouse BA/F3 cells expressing NPM-ALK fusion gene assessed as growth inhibition, IC50 = 0.026 μM.	23837797
KARPAS299	Antiproliferative assay		72 hrs		Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.026 μM.	29174809
NCI-H2228	Antiproliferative assay		72 hrs		Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay, IC50 = 0.026 μM.	30223120
KARPAS299	Cytotoxicity assay		72 hrs		Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay, IC50 = 0.027 μM.	27474925
Ba/F3	Function assay		72 hrs		Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.033 μM.	26568289
NCI-H3122	Antiproliferative assay				Antiproliferative activity against wild type human NCI-H3122 cells, CC50 = 0.038 μM.	26235945
NCI-H3122	Function assay		72 hrs		Inhibition of EML4-ALK in human NCI-H3122 cells assessed as inhibition of cell proliferation after 72 hrs by SRB assay, CC50 = 0.038 μM.	26923695
NCI-H3122	Function assay		72 hrs		Inhibition of EML4-ALK in human NCI-H3122 cells assessed as inhibition of cell proliferation after 72 hrs by SRB assay, CC50 = 0.038 μM.	26923695
NCI-H3122	Function assay		72 hrs		Inhibition of EML4 fused ALK in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB assay, CC50 = 0.038 μM.	28385505
BA/F3	Function assay				Inhibition of ALK (unknown origin) transfected in mouse BA/F3 cells, IC50 = 0.0407 μM.	23837797
Ba/F3	Function assay		72 hrs		Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.041 μM.	26568289
Ba/F3	Function assay		72 hrs		Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.041 μM.	26568289
KARPAS299	Antiproliferative assay		72 hrs		Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.041 μM.	30223120
BAF3	Antiproliferative assay		72 hrs		Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.0549 μM.	29288940
Ba/F3	Function assay		72 hrs		Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.057 μM.	26568289
HCC78	Antiproliferative assay		72 hrs		Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay, IC50 = 0.058 μM.	29174809
HCC78	Antiproliferative assay		72 hrs		Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay, IC50 = 0.058 μM.	30223120
Ba/F3	Function assay		72 hrs		Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.064 μM.	26568289
DFCI76	Antiproliferative assay		72 hrs		Antiproliferative activity against human DFCI76 cells expressing EML4-ALK L1152R mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.072 μM.	26568289
BAF3	Antiproliferative assay				Antiproliferative activity against mouse BAF3 cells expressing ALK L1196M mutant, CC50 = 0.075 μM.	26235945
BA/F3	Function assay		72 hrs		Inhibition of ALK L1196M mutant in mouse BA/F3 cells assessed as inhibition of cell proliferation after 72 hrs by WST1 assay, CC50 = 0.075 μM.	26923695
BA/F3	Function assay		72 hrs		Inhibition of EML4 fused ALK L1196M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay, CC50 = 0.075 μM.	27915169
BA/F3	Function assay		72 hrs		Inhibition of EML4 fused ALK (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay, CC50 = 0.075 μM.	27915169
BAF3	Function assay		72 hrs		Inhibition of ALK L1196M mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by WST-1 assay, CC50 = 0.075 μM.	28385505
KARPAS299	Antiproliferative assay		72 hrs		Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.084 μM.	29288940
SMS-KCNR	Antiproliferative assay		72 hrs		Antiproliferative activity against human SMS-KCNR cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.092 μM.	26568289
NCI-H3122	Antiproliferative assay		72 hrs		Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.096 μM.	29288940
NCI-H2228	Antiproliferative assay		72 hrs		Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay, IC50 = 0.099 μM.	29174809
Ba/F3	Function assay		72 hrs		Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.101 μM.	26568289
NCI-H2228	Cytotoxicity assay		72 hrs		Cytotoxicity against human NCI-H2228 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.1026 μM.	25644671
LAN5	Antiproliferative assay		72 hrs		Antiproliferative activity against human LAN5 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.122 μM.	26568289
SU-DHL1	Antiproliferative assay		72 hrs		Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.122 μM.	29288940
Kelly	Antiproliferative assay		72 hrs		Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.142 μM.	26568289
Ba/F3	Function assay		72 hrs		Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.164 μM.	26568289
SH-SY5Y	Antiproliferative assay		72 hrs		Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.186 μM.	26568289
BAF3	Antiproliferative assay		72 hrs		Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay, IC50 = 0.234 μM.	29288940
SK-N-SH	Antiproliferative assay		72 hrs		Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.303 μM.	26568289
BAF3	Function assay		2 to 3 days		Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 0.3195 μM.	23742252
BA/F3	Cytotoxicity assay				Cytotoxicity against mouse BA/F3 cells transfected with Tel-InsR gene assessed as growth inhibition, IC50 = 0.32 μM.	23837797
SK-N-FI	Antiproliferative assay		72 hrs		Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.349 μM.	26568289
CHLA20	Antiproliferative assay		72 hrs		Antiproliferative activity against human CHLA20 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.363 μM.	26568289
Ba/F3	Function assay		72 hrs		Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.444 μM.	26568289
LAN1	Antiproliferative assay		72 hrs		Antiproliferative activity against human LAN1 cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.549 μM.	26568289
SK-N-BE(2)	Antiproliferative assay		72 hrs		Antiproliferative activity against human SK-N-BE(2) cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.593 μM.	26568289
Ba/F3	Function assay		72 hrs		Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.668 μM.	26568289
BAF3	Antiproliferative assay		72 hrs		Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.726 μM.	29288940
Ba/F3	Function assay		72 hrs		Inhibition of human EGFR del19/T790M/C797S mutant expressed in mouse Ba/F3 cells assessed as cell growth inhibition after 72 hrs by CellTiter-Glo assay, GI50 = 0.7805 μM.	29136465
SK-N-AS	Antiproliferative assay		72 hrs		Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.045 μM.	26568289
BAF3	Cytotoxicity assay		2 to 3 days		Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 2.477 μM.	23742252
Ba/F3	Function assay		72 hrs		Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 2.747 μM.	26568289
BA/F3	Cytotoxicity assay		72 hrs		Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 5.512 μM.	26568289
KARPAS299	Apoptosis assay	60 nM	24 hrs		Induction of apoptosis in human KARPAS299 cells harboring NPM-ALK at 60 nM after 24 hrs by acridine orange/ethidium bromide staining based fluorescence microscopic method	29174809
SU-DHL1	Function assay	20 to 200 nM	1 hr		Inhibition of ALK in human SU-DHL1 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 20 to 200 nM after 1 hr by Western blot analysis	29288940
SU-DHL1	Function assay	20 to 200 nM	1 hr		Inhibition of ALK phosphorylation at Y1278 residue in human SU-DHL1 cells at 20 to 200 nM after 1 hr by Western blot analysis	29288940
NCI-H3122	Function assay	20 to 200 nM	1 hr		Inhibition of ALK in human NCI-H3122 cells assessed as reduction in ERK phosphorylation at T202//Y204 residues at 20 to 200 nM after 1 hr by Western blot analysis	29288940
NCI-H3122	Function assay	20 to 200 nM	1 hr		Inhibition of ALK in human NCI-H3122 cells assessed as reduction in Akt phosphorylation at S473 residue at 20 to 200 nM after 1 hr by Western blot analysis	29288940
SU-DHL1	Function assay	20 to 200 nM	1 hr		Inhibition of ALK in human SU-DHL1 cells assessed as reduction in Akt phosphorylation at S473 residue at 20 to 200 nM after 1 hr by Western blot analysis	29288940
SU-DHL1	Function assay	20 to 200 nM	1 hr		Inhibition of ALK in human SU-DHL1 cells assessed as reduction in ERK phosphorylation at T202//Y204 residues at 20 to 200 nM after 1 hr by Western blot analysis	29288940
NCI-H3122	Function assay	20 to 200 nM	1 hr		Inhibition of ALK phosphorylation at Y1278 residue in human NCI-H3122 cells at 20 to 200 nM after 1 hr by Western blot analysis	29288940
NCI-H3122	Function assay	20 to 200 nM	1 hr		Inhibition of ALK in human NCI-H3122 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 20 to 200 nM after 1 hr by Western blot analysis	29288940
SU-DHL1	Function assay	30 nM	16 hrs		Inhibition of ALK autophosphorylation at Y1507 residue in human SU-DHL1 cells at 30 nM after 16 hrs by Western blot analysis	29627725
SU-DHL1	Function assay	30 nM	16 hrs		Inhibition of ALK in human SU-DHL1 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 30 nM after 16 hrs by Western blot analysis	29627725
NCI-H3122	Function assay	50 to 250 nM	16 hrs		Induction of ALK degradation in human NCI-H3122 cells assessed as decrease in ALK phosphorylation at Y1604 at 50 to 250 nM after 16 hrs by immunoblot method	29660984
SH-SY5Y	Antiproliferative assay		72 hrs		Antiproliferative activity against human SH-SY5Y cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	29660984
CHLA20	Antiproliferative assay		72 hrs		Antiproliferative activity against human CHLA20 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	29660984
SH-SY5Y	Antiproliferative assay		72 hrs		Antiproliferative activity against human SH-SY5Y cells after 72 hrs in presence of ABCB1 inhibitor tariquidar by CellTiter-Glo luminescent cell viability assay	29660984
KARPAS299	Function assay	50 to 250 nM	16 hrs		Induction of ALK degradation in human KARPAS299 cells assessed as decrease in ALK phosphorylation at Y1604 at 50 to 250 nM after 16 hrs by immunoblot method	29660984
CHLA20	Antiproliferative assay		72 hrs		Antiproliferative activity against human CHLA20 cells after 72 hrs in presence of ABCB1 inhibitor tariquidar by CellTiter-Glo luminescent cell viability assay	29660984
NCI-H3122	Antiproliferative assay		72 hrs		Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	29660984
KARPAS299	Antiproliferative assay		72 hrs		Antiproliferative activity against human KARPAS299 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	29660984
SU-DHL1	Antiproliferative assay		72 hrs		Antiproliferative activity against human SU-DHL1 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	29660984
KARPAS299	Apoptosis assay	50 nM	24 hrs		Induction of apoptosis in human KARPAS299 cells assessed as unclear cell shrinkage at 50 nM after 24 hrs by Hoechst 33258 staining based inverted fluorescence microscopy	30223120
KARPAS299	Apoptosis assay	50 nM	24 hrs		Induction of apoptosis in human KARPAS299 cells assessed as late apoptotic cells at 50 nM after 24 hrs by AO/EB double staining based inverted fluorescence microscopy	30223120
KARPAS299	Apoptosis assay	50 nM	24 hrs		Induction of apoptosis in human KARPAS299 cells assessed as fragmentation at 50 nM after 24 hrs by Hoechst 33258 staining based inverted fluorescence microscopy	30223120
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 4 mg/mL (7.16 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.150mg/ml (0.27mM)	Taking the 1 mL working solution as an example, add 50 μL 3 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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Chemical Information, Storage & Stability

Molecular Weight	558.14	Formula	C₂₈H₃₆ClN₅O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1032900-25-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LDK378			Smiles	CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl

Mechanism of Action

Features	Does not cross react with c-Met, and has an improved in vivo glucose homeostasis profile relative to TAE684. May be active in Crizotinib-relapsed tumors.
Targets/IC₅₀/Ki	ALK (Cell-free assay) 0.2 nM Insulin Receptor (Cell-free assay) 7 nM IGF-1R (Cell-free assay) 8 nM STK22D (Cell-free assay) 23 nM FLT3 (Cell-free assay) 60 nM
In vitro	LDK378 shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells.
Kinase Assay	Enzymatic kinase profiling description
Kinase Assay	All kinases are expressed as either Histidine- or GST-tagged fusion proteins using the baculovirus expression technology except for the untagged ERK2 which is produced in E. coli. The kinase activity is measured in the LabChip mobility shift assay. The assay is performed at 30°C for 60 min. The effect of this compound on the enzymatic activity is obtained from the linear progress curves in the absence and presence of this compound and routinely determines from one reading (end point measurement)
In vivo	LDK378 is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. This compound has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. It exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. It induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. This chemical shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23742252/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-ALK / ALK / p-AKT / AKT / p-ERK / ERK pROS1 / ROS1 / pSTAT3 / STAT3		28425916
Growth inhibition assay	Cell viability		29067644

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02450903	Completed	Non-Small-Cell Lung Cancer	Novartis Pharmaceuticals\|Novartis	August 21 2015	Phase 2
NCT02040870	Completed	Non-Small Cell Lung Cancer	Novartis Pharmaceuticals\|Novartis	March 7 2014	Phase 1\|Phase 2
NCT01950481	Completed	Normal Hepatic Function\|Impaired Hepatic Function	Novartis Pharmaceuticals\|Novartis	January 2014	Phase 1
NCT01772797	Completed	Anaplastic Lymphoma Kinase (ALK)\|Non-small Cell Lung Cancer	Novartis Pharmaceuticals\|Novartis	June 2013	Phase 1
NCT01685060	Completed	Non-Small Cell Lung Cancer	Novartis Pharmaceuticals\|Novartis	November 26 2012	Phase 2
NCT01634763	Completed	Tumors Characterized by Genetic Alterations in Anaplastic Lymphoma Kinase (ALK)	Novartis Pharmaceuticals\|Novartis	June 2012	Phase 1

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Frequently Asked Questions

Question 1:
how to reconstitute it for oral administration to mice?

Answer:
It can be resuspended in 30% PEG400/0.5% Tween 80/5% propylene glycol and the suspension can be used for oral gavage feeding.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):