Description
A dual VEGFR and PDGFR family kinase inhibitor (IC50s = 0.002, 0.05, 0.004, and 0.015 µM for VEGFR1, VEGFR2, PDGFRβ, and KIT, respectively); selective for these kinases over FGFR1, EGFR, Src, and c-Met (IC50s = 3.5, >20, 2.5, and 9 µM, respectively); inhibits VEGFR2, PDGFRβ, KIT, and FLT3-ITD phosphorylation in vitro (IC50s = 0.04, 0.02, 0.006, and 0.05 µM, respectively); inhibits PDGF-dependent proliferation of NIH3T3 cells overexpressing PDGFRβ, as well as OC1-AML5 cells expressing wild-type FLT3 and MV4-11 cells carrying the activating FLT3-ITD mutation; inhibits VEGF-induced survival of HUVECs (IC50 = 6.8 nM); reduces tumor growth in human acute myeloid leukemia, renal, and colon cancer, as well as rat glioma, mouse xenograft models when used at doses ranging from 10-80 mg/kg twice per day
Formal name: 5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-(4-morpholinyl)propyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
Synonyms:
Molecular weight: 442.5
CAS: 627908-92-3
Purity: ≥95%
Formulation: A solid
