Aptinib

Min.Order / FOB Price:Get Latest Price

0 Metric Ton	Negotiable

0 Metric Ton

Negotiable

Min.Order :0 Metric Ton
Purity: 99%

Keywords

Aptinib Aptinib Aptinib

Quick Details

Appearance:white powder
Application:Anti-cancer
PackAge:1g/flask
ProductionCapacity:|Metric Ton|Day
Storage:Stored in a cool dry place. It should be protected from heat/light, oxygen and moisture. Keep the container tightly closed
Transportation:By sea. By air

Superiority:

1.We are specializing in providing customers with complete chemical raw materials.
2.Superior quality, moderate price & quick delivery.
3. Extensive international cooperation experience.
4. Outstanding communication skills.

Details:

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 μM, 0.429 μM and 0.53 μM, respectively. Apatinib inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50 = 0.17μM). 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. 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 iodoarylazidoprazosin in a concentration-dependent manner.

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