Description
A dual inhibitor of Kit (IC50s = 80 and 629 nM for the actived and non-activated kinase, respectively, in cell-free assays) and the kinase insert domain receptor (KDR; IC50 = 9 nM); selective for these kinases over a panel of 13 additional kinases (IC50s = 1.3->10 µM) but also inhibits FLT1, CSF1R, C-RAF, and LCK (IC50s = 8, 15, 41, and 22 nM, respectively); inhibits Kit autophosphorylation in NCI-H526 and HMC-1 cells expressing wild-type Kit and Kit containing the constitutively active KitV560G mutation, respectively, and stem cell factor-induced Kit autophosphorylation in NCI-H526 cells expressing wild-type Kit (IC50s = 58.1 and 78.9 nM, respectively); inhibits VEGF-induced autophosphorylation of VEGFR2 in HUVECs (IC50 = 64.4 nM); decreases endothelial sprout formation by >50% in isolated rat aortic rings at 100 nM; reduces tumor growth in a variety of mouse xenograft models at 200 mg/kg per day
Formal name: 3-[(4-quinolinylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]-2-thiophenecarboxamide
Synonyms:
Molecular weight: 443.4
CAS: 728033-96-3
Purity: ≥98%
Formulation: A crystalline solid
