Apatinib (Rivoceranib, YN968D1)

Description: Apatinib (formerly known as Rivoceranib, YN-968D1) is a potent, orally bioavailable, and selective inhibitor of the VEGF (vascular endothelial growth factor receptor) signaling pathway with potential antiangiogenic and antineoplastic activities. It inhibits VEGFR2 with an IC50 of 1 nM. Apatinib (Aitan, trade name in China) was approved by the Chinese FDA (CFDA) in December 2014 foe the treatment of late-stage gastric carcinoma. Apatinib potently suppressed the kinase activities of VEGFR-2, c-kit and c-src, and inhibited cellular phosphorylation of VEGFR-2, c-kit and PDGFRbeta. Apatinib effectively inhibited proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. In vivo, Apatinib alone and in combination with chemotherapeutic agents effectively inhibited the growth of several established human tumor xenograft models with little toxicity.

References: Cancer Sci. 2011; 102(7):1374-80; Cancer Res. 2010; 70(20):7981-91; Biochem Pharmacol. 2012; 83(5):586-97.

Related CAS: 811803-05-1 (free base); 1218779-75-9 (mesylate)

Chemical Name: N-(4-(1-cyanocyclopentyl)phenyl)-2-((4-methylpyridin-3-yl)amino)nicotinamide

InChi Key: MGZNERAVOCFMCU-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H23N5O/c1-17-10-14-26-15-21(17)29-22-20(5-4-13-27-22)23(30)28-19-8-6-18(7-9-19)24(16-25)11-2-3-12-24/h4-10, 13-15H, 2-3, 11-12H2, 1H3, (H, 27, 29)(H, 28, 30)

SMILES Code: O=C(NC1=CC=C(C2(C#N)CCCC2)C=C1)C3=C(NC4=C(C)C=CN=C4)N=CC=C3