供货周期: | 一周 |
品牌: | 爱必信 |
规格: | ≥98% |
货号: | abs812083 |
CAS号: | 552325-73-2 |
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抑制剂描述: 产品名称:A-674563 产品别名:见爱必信官网 英文别名:A-674563 靶点:Akt CAS:552325-73-2 纯度:≥98% 外观:见爱必信官网 保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述: A-674563 is a potent and selective Akt1 inhibitor with a Ki of 11 nM. 溶解性:DMSO :72 mg/mL (200.87 mM) 体外研究: A-674563 is achieved from A-443654 by replacing the indole with a phenyl moiety and getting oral activity. A-674563 slows proliferation of tumor cells with EC50 of 0.4 μM. A-674563 does not inhibit Akt phosphorylation per se, but blocks the phosphorylation of Akt downstream targets in a dose-dependent manner. A-674563 induced Akt blockade results in decreased STS cell downstream target phosphorylation and tumor cell growth inhibiton. A-674563 induces G2 cell cycle arrest and apoptosis in STS cells. 体内研究:20 mg/kg A-674563 increases plasma insulin in an oral glucose tolerance test. A-674563 shows no significant monotherapy tumor inhibitory activity; the efficacy of the combination therapy is significantly improved compared to paclitaxel monotherapy. A674563-treated (20 mg/kg/bid, p.o.) mice exhibits slower tumor growth and more than 50% decrease in the tumor volume at the termination of the study compared with that in control group. A-674563 is identified to have drastically improved PK profile with oral bioavailability of 67% in mouse, but is 70-fold less active than A-443654.
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