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產品描述： 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. |
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靶點：
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：
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. |
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溶解性：
DMSO : 125 mg/mL (291.43 mM; Need ultrasonic) |
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保存條件：
-20℃ |
配置溶液濃度參考：
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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 |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京