- Product Details
Keywords
- Aptinib
- Aptinib
- Aptinib
Quick Details
- ProName: Aptinib
- CasNo: 811803-05-1
- Appearance: white powder
- Application: Anti-cancer
- DeliveryTime: 5 days after receive LC or TT
- PackAge: 1g/flask
- Port: shanghai
- ProductionCapacity: Metric Ton/Day
- Purity: 99%
- Storage: Stored in a cool dry place. It should ...
- Transportation: By sea. By air
- LimitNum: 0 Metric Ton
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.