Description
An ATP-competitive inhibitor of human VEGFR1 and 2 and FGFR1 (IC50s = 380, 25, and 148 nM, respectively, for the human recombinant proteins); selective for VEGFR1 and 2 and FGFR1 over PDGFRβ, EGFR, LCK, PKCα, and JAK3 (IC50s = >1,900 nM; inhibits recombinant mouse Flk1 (IC50 = 89 nM); inhibits VEGF- and FGF-stimulated proliferation of HUVECs in vitro (IC50s = 40 and 276 nM, respectively); inhibits tumor growth by 85% and 97% when administered at 60 and 90 mg/kg p.o., respectively, for 10 days in an H3396 breast cancer mouse xenograft model; inhibits bile duct ligation-induced liver fibrosis in mice (25 mg/kg per day for 7 days, p.o.) and increases expression of PDGFβ, PDGFRβ, TGF-β1, TGF-β R2, FGF2, FGFR2, and VEGFR2 mRNAs
Formal name: (2R)-1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol
Synonyms: BMS 540215
Molecular weight: 370.4
CAS: 649735-46-6
Purity: ≥95%
Formulation: A crystalline solid
Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Immunology & Inflammation
