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上海源葉生物科技有限公司
主營產品： S30260異硫氰酸胍,30259鹽酸胍,嗜熱菌蛋白酶 |
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- 聯系人：
- 何小姐
- 電話：
- 86-021-61559134
- 手機：
- 15921386130
- 傳真：
- 86-021-55068248
- 地址：
- 上海市松江區長塔路465號6幢
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- 200433
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- www.shyuanye.com
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更新時間：2024-07-04 07:11:16瀏覽次數：139
聯系我們時請說明是化工儀器網上看到的信息，謝謝!
- 提示：詳情請下載說明書。
- 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.
- 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
- 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.
- 溶解度： 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：部分產品我司僅能提供部分信息，我司不保證所提供信息的性，僅供客戶參考交流研究之用。
