AT7867 dihydrochloride
| CAS号 | 1431697-86-7 | 货号 | BCP30936 |
| 中文名 | AT7867 dihydrochloride | ||
| 英文名 | AT7867 dihydrochloride | ||
| 中文别名 | |||
| 英文别名 | AT 7867 Dihydrochloride; AT-7867 Dihydrochloride;AT7867 2HCl; | ||
| 分子式 | C20H20ClN3.2(HCl) | 分子量 | 410.77 |
| 生物活性 | 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. 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. | ||
| 信号通路 | GPCR/G Protein Wnt/Stem Cell PI3K/Akt/mTOR MAPK Pathway | ||
| 靶 点 | PKA RSK AKT | ||
结构式
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