Apatinib

Apatinib is a tyrosine kinase inhibitor that potently suppresses the kinase activity of vascular endothelial growth factor 2 (VEGFR2, IC50 = 1 nM). It is less effective against c-kit (IC50 = 429 nM), Ret (IC50 = 13 nM), and c-src (IC50 = 53 nM) and does not inhibit EGFR, Her-2, or FGFR1 (IC50s = >10 µM). Apatinib has been shown to inhibit the proliferation, migration, and tube formation of human umbilical vein endothelial cells stimulated by fetal bovine serum and, either alone, or in combination with chemotherapeutic agents, prevented the growth of several established human tumor xenograft models.Formal Name: N-[4-(1-cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide. CAS Number: 811803-05-1. Synonyms: YN968D1. Molecular Formula: C24H23N5O. Formula Weight: 397.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 1 mg/ml. lambdamax: 236, 261, 345 nm. SMILES: O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC=C(C4(C#N)CCCC4)C=C3. InChi Code: InChI=1S/C24H23N5O/c25-17-24(11-1-2-12-24)19-5-7-20(8-6-19)29-23(30)21-4-3-13-27-22(21)28-16-18-9-14-26-15-10-18/h3-10,13-15H,1-2,11-12,16H2,(H,27,28)(H,29,30). InChi Key: WPEWQEMJFLWMLV-UHFFFAOYSA-N.