S80038
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- 公司名稱 上海源葉生物科技有限公司
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- 廠商性質(zhì) 生產(chǎn)廠家
- 更新時間 2024/7/3 19:08:54
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- 產(chǎn)品描述： MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy
- 靶點(diǎn)： Akt1:8 nM (IC50);Akt2:12 nM (IC50);Akt3:65 nM (IC50)
- 體內(nèi)研究： Both MK-2206 dihydrochloride (MK-2206 (2HCl)) doses (oral gavage; 480 mg/kg once a week and 240 mg/kg three times a week; for 2 weeks) can inhibit the growth of human CNE-2 xenografts in nude mice. No other obvious toxicity is observed in mice. MK-2206 dihydrochloride (orally; 120 mg/kg; alternate days; for 3 weeks) significantly inhibits tumor growth in 3-5 week old athymic nude mice with GEO colon carcinoma cells.
- 參考文獻(xiàn)：
1. Li Yan, et al. Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor. 2009.2. Xing Y, et al. Phase II trial of AKT inhibitor MK-2206 in patients with advanced breast cancer who have tumors with PIK3CA or AKT mutations, and/or PTEN loss/PTEN mutation. Breast Cancer Res. 2019 Jul 5;21(1):78.3. Zhao YY, et al. Effects of an oral allosteric AKT inhibitor (MK-2206) on human nasopharyngeal cancer in vitro and in vivo. Drug Des Devel Ther. 2014 Oct 10;8:1827-37.4. Agarwal E, et al. Akt inhibitor MK-2206 promotes anti-tumor activity and cell death by modulation of AIF and Ezrin in colorectal cancer. BMC Cancer. 2014 Mar 1;14:145.
- 溶解度： DMSO : 16.67 mg/mL (34.70 mM; ultrasonic and warming and heat to 70°C) H2O : 3.57 mg/mL (7.43 mM; ultrasonic and warming and heat to 60°C)
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 2.082 ml 10.408 ml 20.816 ml 5 mM 0.416 ml 2.082 ml 4.163 ml 10 mM 0.208 ml 1.041 ml 2.082 ml 50 mM 0.042 ml 0.208 ml 0.416 ml
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