XL184

XL184 is an inhibitor of VEGFR2 (IC50 = 0.035 nM). It is selective for VEGFR2 over Ron, EGFR, IGF-1R, and EphA4/B4, but also inhibits c-Met, RET, c-Kit, Axl, FLT3, and Tie2 (IC50s = 1.3, 5.2, 4.6, 7, 11.3, and 14.3 nM, respectively). XL184 (4.6 nM) inhibits VEGF-induced tubule formation in human microvascular endothelial cells (HMVECs). It reduces migration and invasion of B16/F10 melanoma cells induced by hepatocyte growth factor (HGF) when used at a concentration of 123 nM. XL184 (60 mg/kg) induces tumor regression in an MDA-MB-231 breast cancer mouse xenograft model. Unlike sunitinib (Cay-13159), XL184 does not increase the number of pulmonary tumor foci in an MDA-MB-231 mouse metastasis model. It also protects primary placental fibroblasts from Zika virus infection. Formulations containing XL184 have been used in the treatment of renal cell and hepatocellular carcinomas.Formal Name: N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide. CAS Number: 849217-68-1. Synonyms: BMS-907351, Cabozantinib. Molecular Formula: C28H24FN3O5. Formula Weight: 501.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 5 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml, Ethanol: 2 mg/ml. lambdamax: 242, 308, 322 nm. SMILES: COC1=C(OC)C=C(C(OC2=CC=C(NC(C3(C(NC4=CC=C(F)C=C4)=O)CC3)=O)C=C2)=CC=N5)C5=C1. InChi Code: InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34). InChi Key: ONIQOQHATWINJY-UHFFFAOYSA-N.