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BMS-794833

BMS-794833

Item no.	S2201-50
Manufacturer	Selleckchem
CASRN	1174046-72-0
Amount	50 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 200 mg 5 mg 50 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Brain Cancer
Type	Inhibitors
Specific against	other
Smiles	C1=CC(=CC=C1C2=CNC=C(C2=O)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F)F
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	1174046-72-0'
Similar products	BMS
Available
Manufacturer - Targets	MET
Storage Conditions	2 years -80 in solvent
Molecular Weight	468, 84
Administration	Orally once daily
Animal Models	GTL-16 and U87 xenografts
Cell lines	GTL-16 cells
Clinical Trials	BMS798433 is currently in Phase I clinical trial against advanced or metastatic solid tumor.
Concentrations	ca. 1 uM
Dosages	25 mg/kg
IC50	1.7 nM, 1.7 nM, 1.7 nM, 1.7 nM, 1.7 nM, 1.7 nM
In vitro	BMS794833 also inhibits Met receptor activated gastric carcinoma cell line, GTL-16, with IC50 of 39 nM. [1]
In vivo	In GTL-16 human gastric tumor xenografts model, BMS798433 shows greater than 50% TGI for at least one tumor doubling time with no overt toxicity observed during 14 days. BMS798433 also shows complete tumor stasis at a dose of 25 mg/kg against U87 glioblastoma model. [1]
Incubation Time	72 hours
Kinase Assay	Met kinase assay, BMS798433 is dissolved in DMSO and diluted by water before use. The reaction solution contains baculovirus expressed GST-Met kinase, 20 mM Tris-HCl (pH 7.4), 1 mM MnCl2, 1 mM DTT, 0.1mg BSA, 0.1 mg polyGlu4/tyr, 1uM ATP and 0.2uCi gammaâ€“ATP. Reactions are incubated at 30 C for 1 hour and stopped by 8% TCA. TCA precipitates are collected onto GF/C plates using a universal harvester and the filters are quantitated using liquid scintillation counter.
Method	GTL-16 cells are seeded into 96 well plates and incubated for 24 hours. BMS798433 is dissolved in DMSO at 10 mM and diluted with culture medium before use. Then BMS798433 is added to the cells for 72 hours. After that, MTS assay is used to measure the IC50.
Solubility (25C)	DMSO 94 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.
Chemical Name	N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-5-(4-fluorophenyl)-4-oxo-1, 4-dihydropyridine-3-carboxamide

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

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S2201-50-datasheet.pdf

S2201-50-safety-datasheet.pdf