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.
仅供研究使用。 我们不向患者出售。
名称 | Apatinib |
---|---|
Iupac 化学名称 | Apatinib |
同义词 | YN968D1 |
英文同义词 | YN968D1 |
分子式 | C25H27N5O4S |
分子量 | 493.58 |
Smile | Cc1ccncc1Nc2c(cccn2)C(=O)Nc3ccc(cc3)C4(CCCC4)C#N.CS(=O)(=O)O |
InChiKey | BDGPIQYIFFSTGI-UHFFFAOYSA-N |
InChi | 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) |
Cas号 | 811803-05-1 |
MDL | MFCD22124899 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
---|---|---|---|---|
大货 | 询价 | 询价 | 询价 |