S81216 |
AZD5363 |
源葉(MedMol) | 97% |
- 提示:詳情請下載說明書。
- 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: 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:
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
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輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)