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Apatinib

编号: 17022301
Cas号: 811803-05-1
纯度: 98% 

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。

化学信息

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 
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)
Cas号811803-05-1
MDLMFCD22124899
相关CAS号

订购信息

包装价格库存纯度备货期
大货询价询价询价
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外观性状off-white solid 
纯度98% 
存储3 years -20ºCpowder 
可溶性Soluble in DMSO 
处理方式
运输条件Shipped under ambient temperature as non-hazardous chemical. 
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study
Not available

化学结构

17022301 - Apatinib | CAS 811803-05-1

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