A-674563

A-674563

参考价:¥1213
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)
Water :72 mg/mL (200.87 mM)
Ethanol :18 mg/mL (50.21 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.

产品信息订购:

  产品货号   产品名称   规格 价格 大包装及货期
  abs812083   A-674563   2mg   1213.00   立即咨询
  abs812083   A-674563   5mg   2097.00   立即咨询
  abs812083   A-674563   10mg   3275.00   立即咨询

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