Axitinib

Axitinib is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively). It also inhibits c-Kit and PDGFRbeta (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs). Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.Formal Name: N-methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide. CAS Number: 319460-85-0. Synonyms: AG-013736. Molecular Formula: C22H18N4OS. Formula Weight: 386.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.25 mg/ml, DMSO: 2.5 mg/ml. lambdamax: 259, 332 nm. SMILES: O=C(NC)C1=C(SC2=CC3=C(C(/C=C/C4=NC=CC=C4)=NN3)C=C2)C=CC=C1. InChi Code: InChI=1S/C22H18N4OS/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14H,1H3,(H,23,27)(H,25,26)/b12-9+. InChi Key: RITAVMQDGBJQJZ-FMIVXFBMSA-N.