| 產(chǎn)品描述： | Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively. |
| 靶點(diǎn)： |
Akt1:3 nM (IC50);Akt2:7 nM (IC50);Akt3:7 nM (IC50);ROCK2:60 nM (IC50);ROCK1:470 nM (IC50);PKA:7 nM (IC50);P70S6K:6 nM (IC50);Autophagy;Akt;?PKA;?mTOR;?Autophagy |
| 體內(nèi)研究： |
Oral dosing of Capivasertib (AZD5363) to nude mice causes dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC50?~0.1 μM total plasma exposure), reversible increases in blood glucose concentrations, and dose-dependent decreases in 2[18F]fluoro-2-deoxy-D-glucose (18F-FDG) uptake in U87-MG xenografts. Chronic oral dosing of Capivasertib caused dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+?breast cancer models. Capivasertib also significantly enhances the antitumor activity of RP-56976 and GW572016 in breast cancer xenografts |
| 參考文獻(xiàn)： |
1. Davies BR, et al. Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Mol Cancer Ther. 2012 Apr;11(4):873-87. |
| 溶解性： |
DMSO : 125 mg/mL (291.43 mM; Need ultrasonic) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.331 ml |
11.657 ml |
23.314 ml |
| 5 mM |
0.466 ml |
2.331 ml |
4.663 ml |
| 10 mM |
0.233 ml |
1.166 ml |
2.331 ml |
| 50 mM |
0.047 ml |
0.233 ml |
0.466 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶(hù)參考交流研究之用。 |
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