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Apatinib Catalog No : 17022301

Chemical Information

Product NameApatinib
Iupac Chemical NameApatinib 
SynonymsYN968D1 
Molecular FormulaC25H27N5O4S 
Molecular Weight493.58 
SmileCc1ccncc1Nc2c(cccn2)C(=O)Nc3ccc(cc3)C4(CCCC4)C#N.CS(=O)(=O)O
InChiKeyBDGPIQYIFFSTGI-UHFFFAOYSA-N
InChiInChI=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)
Cas811803-05-1
MDLMFCD22124899

Technical Data

Appearanceoff-white solid 
Purity98% 
SolubilitySoluble in DMSO 
Storage3 years -20ºCpowder 
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
Quality control

Description

Apatinib is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.

Apatinib (YN968D1) is a novel, orally bioavailable, selective inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits VEGFR2. Apatinib can also potently suppress the activities of Ret, c-kit and c-src with IC50 of 0.013 M, 0.429 M and 0.53 M, respectively. Apatinib inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFR. Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50 = 0.17M). Apatinib effectively inhibits proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. [1] Apatinib reverses ABCB1- and ABCG2-mediated MDR by inhibiting their transport function, but not by blocking the AKT or ERK1/2 pathway or downregulating ABCB1 or ABCG2 expression. Apatinib significantly potentiates the cytotoxicity of established ABCB1 and ABCG2 substrates and increased the accumulation of DOX and Rho 123 in ABCB1- or ABCG2-overexpressing cells. Furthermore, apatinib significantly inhibited the photoaffinity labeling of both ABCB1 and ABCG2 with [125I]iodoarylazidoprazosin in a concentration-dependent manner.

 

Chemical Structure

17022301 - Apatinib | CAS 811803-05-1

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