货号	规格	价格	上海	北京	武汉	南京
S81021-5mg	≥98%	￥144.00 S81021-5mg ￥144.00 现货	10 10	-	-	-
S81021-10mg	≥98%	￥272.00 S81021-10mg ￥272.00 现货	10 10	-	-	-
S81021-50mg	≥98%	￥669.00 S81021-50mg ￥669.00 现货	9 9	-	-	-

货号

规格

价格

上海

北京

武汉

南京

购买数量

S81021-5mg

≥98%

￥144.00

S81021-10mg

≥98%

￥272.00

S81021-50mg

≥98%

￥669.00

产品描述：

AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.

靶点：

Akt2:17 nM (IC50);p70S6K:85 nM (IC50);Akt1:32 nM (IC50);Akt3:47 nM (IC50);PKA:20 nM (IC50);Akt; PKA; S6Kinase

体内研究：

In vivo: Following oral administration at 20 mg/kg, the elimination of AT7867 from plasma appears 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

参考文献：

1. Grimshaw KM, et al. AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. Mol Cancer Ther, 2010, 9(5), 1100-1110.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.96 ml	14.799 ml	29.598 ml
5 mM	0.592 ml	2.96 ml	5.92 ml
10 mM	0.296 ml	1.48 ml	2.96 ml
50 mM	0.059 ml	0.296 ml	0.592 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶(AT7867)

AT7867

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)