Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AT7867 dihydrochloride 是一种有效的ATP 竞争性的Akt1/Akt2/Akt3和p70S6K/PKA 抑制剂,IC50值分别为 32 nM/17 nM/47 nM 和 85 nM/20 nM,具有癌症治疗的潜力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 591 | 5日内发货 | ||
5 mg | ¥ 997 | 5日内发货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,090 | 5日内发货 |
AT7867 dihydrochloride 的其他形式现货产品:
产品描述 | AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1 / Akt2 / Akt3 and p70S6K / PKA kinase with IC 50 s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively. AT7867 dihydrochloride is able to induce pharmacodynamic changes and inhibit human tumor xenograft growth. |
体外活性 | AT7867 ATP-competitive inhibited AKT2 with the Ki of 18nM. AT7867 also shows potent activity against the structurally related AGC kinases p70S6K and PKA, but shows a clear window of selectivity against kinases from other kinase sub-families. In vitro growth inhibition studies show that AT7867 blocks proliferation in a number of human cancer cell lines. AT7867 appears to be most potent at inhibiting proliferation in MES-SA uterine, MDA-MB-468 and MCF-7 breast, and HCT116 and HT29 colon lines (IC 50 values range from 0.9-3 μM), and least effective in the two prostate lines tested (IC 50 values range from 10-12 μM) [1]. |
体内活性 | Following oral administration at 20 mg/kg, the elimination of AT7867 from plasma seems to be similar to that observed after i.v. administration. Plasma levels of AT7867 remain above 0.5 μM for at least 6 hours following an oral dose of 20 mg/kg. Assuming linear pharmacokinetics following i.v. administration, the bioavailability by the oral route is calculated to be 44%. In vivo pharmacodynamic (PD) biomarker studies are therefore performed with this model. Following pharmacokinetic and tolerability studies, doses of AT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) are administered to athymic mice bearing MES-SA tumors and the phosphorylation status of GSK3β and S6RP in tumors is monitored over time. Clear inhibition of phosphorylation of the two markers of pathway activity is seen at 2 and 6 hours following treatment with AT7867. By 24 hours, total levels of both GSK3β and S6RP are greatly reduced [1]. |
分子量 | 410.77 |
分子式 | C20H22Cl3N3 |
CAS No. | 1431697-86-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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