货号	规格	价格	上海	北京	珠海	重庆	武汉
S83288-5mg	≥99%	￥1190.00 S83288-5mg ￥1190.00 3-5天	0 货期：3-5天	-	-	-	-
S83288-10mg	≥99%	￥1590.00 S83288-10mg ￥1590.00 3-5天	0 货期：3-5天	-	-	-	-
S83288-50mg	≥99%	￥3290.00 S83288-50mg ￥3290.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

AT7867 dihydrochloride 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)

体外研究：

The inhibition of AKT2 by AT7867 is shown to be ATP-competitive with a Ki of 18nM. AT7867 also displays 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 (IC50 values range from 0.9-3 μM), and least effective in the two prostate lines tested (IC50 values range from 10-12 μM)

体内研究：

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、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.434 ml	12.172 ml	24.345 ml
5 mM	0.487 ml	2.434 ml	4.869 ml
10 mM	0.243 ml	1.217 ml	2.434 ml
50 mM	0.049 ml	0.243 ml	0.487 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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AT7867 (dihydrochloride)