产品信息
抗原名称
Akt2 ,PKA ,Akt1 ,Akt3 ,p70 S6K
商品描述
AT-7867是一种有效的，ATP竞争性的Akt1/2/3和p70S6K/PKA抑制剂，无细胞试验中IC50分别为32 nM/17 n/47 nM和85 nM/20 nM，对AGC激酶家族以外几乎没有抑制活性。
分子量
337.85
纯度
＞98%
可溶性
DMSO 68 mg/mL (201.27 mM)
Ethanol 5 mg/mL (14.79 mM)
Water Insoluble
Ethanol 5 mg/mL (14.79 mM)
Water Insoluble
In vitro(体外研究)
AT7867 also inhibits structurally related AGC kinases p70S6K and PKA with IC50 of 20 nM and 85 nM, respectively. AT7867 shows ATP-competitive activity to Akt2 with Ki of 18 nM. AT7867 exhibits antiproliferation in cell lines with PTEN or PIK3CA mutations and shows great potent to MES-SA, MDA-MB-468, MCF-7, HCT116 and HT29 with IC50 of 0.94 μM, 2.26 μM, 1.86 μM, 1.76 μM and 3.04 μM, respectively. AT7867 also suppresses the cell growth of U87MG, PC-3 and DU145 cells with IC50 of 8.22 μM, 10.37 μM and 11.86 μM, respectively. AT7867 suppresses Akt activity by inhibiting phosphorylation of GSK-3β in human tumor cells with IC50 of 2-4 μM. AT7867 also induces the phosphorylation of the following Akt direct substrates including proapoptotic transcription factors FKHR (FoxO1a), FKHRL1 (FoxO3a) and the downstream target S6RP in U87MG cells.
In vivo(体内研究)
AT7867 shows bioavailability of 44% in mice by p.o. route. AT7867 could increase the cleaved PARP in MES-SA xenografts at 20 mg/kg i.p. or 90 mg/kg p.o.. AT7867 significantly inhibits the tumor growth in MES-SA xenografts or U87MG xenografts with T/C of 0.37 and 0.51, respectively.
背景
别名
AT7867; AT 7867
分子式
C20H20ClN3
CAS号
857531-00-1
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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