1174046-72-0

Basic information

• Product Name: BMS-794833
• Synonyms: BMS-794833;3-PyridinecarboxaMide, N-[4-[(2-aMino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-5-(4-fluorophenyl)-1,4-dihydro-4-oxo-;N-[4-((2-Amino-3-chloropyridin-4-yl)oxy)-3-fluorophenyl]-5-(4-fluorophenyl)-4-oxo-1,4-dihydropyridine-3-carboxamide;N-[4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl]-5-(4-fluorophenyl)-4-oxo-1,4-dihydropyridine-3-carboxamide;MS-794833;N-[4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl]-5-(4-fluorophenyl)-4-oxo-1,4-dihydropyridine-3-carboxamide MS-794833;N-[4-(2-AMINO-3-CHLOROPYRIDIN-4-YL)OXY-3-FLUOROPHENYL]-5-(4-FLUOROPHENYL)-4-OXO-1H-PYRIDINE-3-CARBOXAMIDE;PDYXPCKITKHFOZ-UHFFFAOYSA-N
• CAS NO: 1174046-72-0
• Molecular Formula: C₂₃H₁₅ClF₂N₄O₃
• Molecular Weight: 468.8400064
• Product Categories: Inhibitors
• Mol File: 1174046-72-0.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 637.2±55.0 °C(Predicted)
• Appearance: /
• Density: 1.508
• Solubility: ≥23.45 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
• PKA: 8.79±0.69(Predicted)
• CAS DataBase Reference: BMS-794833(CAS DataBase Reference)
• NIST Chemistry Reference: BMS-794833(1174046-72-0)
• EPA Substance Registry System: BMS-794833(1174046-72-0)

Safety Data

• Hazardous Substances Data: 1174046-72-0(Hazardous Substances Data)

Usage

Uses

BMS-794833 is a potent ATPcompetitive Met/VEGFR-2 kinase inhibitor and it also inhibits Ron (Met family),Axl and Flt-3 with IC50 values <3 nM.

Biological Activity

bms-794833 is a potent atp competitive, dual inhibitor of c-met and vegfr2 (ic50 = 1.7 nm and 15 nm, respectively). it also has inhibitory effect on ron, axl and flt3 (ic50 < 3 nm).c-met, also called met, is a membrane receptor that is essential for embryonic development and wound healing. vegfr are receptors for vascular endothelial growth factor and belong to receptor tyrosine kinases. it mediates in various cellular functions, including endothelial proliferation, migration, survival, tubular morphogenesis and sprouting. [1]bms794833 also inhibited gastric cancer cell line (gtl-16) that induced by c-met receptor, gtl-16, ic50 = 39 nm [1]. in human gastric tumor xenografts model, bm798433 exhibits > 50% tgi for at least one tumor doubling time without significant toxicity in 14 days. in u87 glioblastoma model, 25mg/kg of bms798433 exert complete tumor stasis. [1]

references

[1] 4-pyridinone compounds and their use of cancer, borzilleri et al, united states patent application publication, pub no. : us 2012/0114643 a1, pub.date: may 10, 2012.

Upstream product

• 1174047-03-0 N-(4-(3-chloro-2-(diphenylmethyleneamino)pyridin-4-yloxy)-3-fluorophenyl)-5-(4-fluorophenyl)-4-oxo-1,4-dihydropyridine-3-carboxamide 

Relevant articles and documents

4-PYRIDINONE COMPOUNDS AND THEIR USE FOR CANCER

Disclosed are compounds of Formula (I)and salts thereof. Also, disclosed are methods of using the compounds in the treatment of proliferative diseases, such as cancer, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a