Description
Description: IC50: 1.7 nM/15 nM for Met/VEGFR2 The signaling pathway of the receptor tyrosine kinase MET and its ligand hepatocyte growth factor is important for cell growth, survival, and motility and is functionally linked to the signaling pathway of VEGF, which is widely recognized as a key effector in angiogenesis and cancer progression. BMS-817378 is a potent ATP competitive inhibitor of Met/VEGFR2. In vitro: BMS-794833, which is the active moiety of BMS-817378, is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM. BMS-794833 also inhibits Met receptor activated gastric carcinoma cell line, GTL-16, with IC50 of 39 nM . In vivo: BMS-798433 shows greater than 50% TGI for at least one tumor doubling time with no toxicity observed during 14 days in GTL-16 human gastric tumor xenografts model. BMS-798433 also shows complete tumor stasis at 25 mg/kg against U87 glioblastoma model . Clinical trial: BMS-817378 is now in its ascending multiple-dose study in subjects with advanced cancers.
Product information
CAS Number: 1174161-69-3
Molecular Weight: 578.85
Formula: C24H18ClF2N4O7P
Chemical Name: (Z)-N-{4-[(3-chloro-2-imino-1,2-dihydropyridin-4-yl)oxy]-3-fluorophenyl}-5-(4-fluorophenyl)-4-oxo-1-[(phosphonooxy)methyl]-1,4-dihydropyridine-3-carboximidic acid
Smiles: N=C1NC=CC(OC2C=CC(=CC=2F)/N=C(\O)/C2=CN(COP(O)(O)=O)C=C(C3=CC=C(F)C=C3)C2=O)=C1Cl
InChiKey: KXDZWUPUSDCGDD-UHFFFAOYSA-N
InChi: InChI=1S/C24H18ClF2N4O7P/c25-21-20(7-8-29-23(21)28)38-19-6-5-15(9-18(19)27)30-24(33)17-11-31(12-37-39(34,35)36)10-16(22(17)32)13-1-3-14(26)4-2-13/h1-11H,12H2,(H2,28,29)(H,30,33)(H2,34,35,36)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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