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• 產(chǎn)品描述： Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.

• 靶點(diǎn)： mTOR:2.81 nM (IC50);mTORC1;mTORC2;PI3Kα:3.766 μM (IC50);Autophagy;Apoptosis;Akt;PI3K;S6Kinase;mTOR;Autophagy

• 體內(nèi)研究：
  Vistusertib (AZD2014) induces dose-dependent tumor growth inhibition in several xenograft and primary explant models. The antitumor activity of Vistusertib (AZD2014) is associated with modulation of both mTORC1 and mTORC2 substrates, consistent with its mechanism of action. The pharmacokinetics of Vistusertib (AZD2014) in mice is tested upon administration of doses between 7.5 and 15 mg/kg. A dose-dependent increase in Cmax and AUC is observed following single dose and repeat dosing of AZD2014: Cmax range from 1 to 16 μM and AUC range from 220 to 5,042 μM·h across this dose range. The pharmacodynamic effect of Vistusertib (AZD2014) against an mTORC1 biomarker (phosphorylation of S6) and an mTORC2 biomarker (phosphorylation of AKT) is assessed in SCID mice bearing MCF7 xenografts following administration of 3.75, 7.5, and 15 mg/kg AZD2014. There is a good relationship between the drug plasma concentrations and biomarker levels (estimated p-AKT IC50 of 0.119 μM total, 53% SE, and estimated p-S6 IC50 0.392 μM, 28.8% SE)

• 參考文獻(xiàn)：
  1. Guichard SM, et al. AZD2014, an inhibitor of mTORC1 and mTORC2, is highly effective in ER+ breast cancer when administered using intermittent or continuous schedules. Mol Cancer Ther. 2015 Nov;14(11):2508-18.

• 溶解性： DMSO  :  ≥  50  mg/mL  (108.10  mM)

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.162 ml	10.81 ml	21.62 ml
  5 mM	0.432 ml	2.162 ml	4.324 ml
  10 mM	0.216 ml	1.081 ml	2.162 ml
  50 mM	0.043 ml	0.216 ml	0.432 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，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)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)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *