apatinib-mesylate

Description: Apatinib mesylate, the mesylate salt of apatinib, is a potent, orally bioavailable, and selective inhibitor of the VEGF (vascular endothelial growth factor receptor) signaling pathway with IC50 of 1 nM for VEGFR2. It has potential antiangiogenic and antineoplastic activities. 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. A phase I study of Apatinib has shown encouraging antitumor activity and a manageable toxicity profile. These findings suggest that Apatinib has promise as an antitumor drug and might have clinical benefits.

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)

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

InChi Key: BDGPIQYIFFSTGI-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H23N5O.CH4O3S/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; 1-5(2, 3)4/h4-10, 13-15H, 2-3, 11-12H2, 1H3, (H, 27, 29)(H, 28, 30); 1H3, (H, 2, 3, 4)

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