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  • A-674563 hydrochloride
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A-674563 hydrochloride

An Akt inhibitor

原价
¥1025-12462
价格
820-9970
A-674563 hydrochloride的二维码

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  • 库存: 现货
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  • 货号: ajcx13684
  • CAS: 2070009-66-2
  • 别名:
  • 分子式: C22H23ClN4O
  • 分子量: 394.9
  • 纯度: >98%
  • 溶解度: H2O:100 mg/mL (253.23 mM; Need ultrasonic); DMSO:62.5 mg/mL (158.27 mM; Need ultrasonic)
  • 储存: -20°C, stored under nitrogen
  • 库存: 现货

Background

Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival, as well as angiogenesis. A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki = 11 nM for Akt1).1 It shows inhibitory activity against PKA and Cdk2 with IC50 values of 16 and 46 nM, respectively, but is 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families.1 A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4 ?M.1 In vivo, 40 mg/kg/day A-674563 in combination with 15 mg/kg/day paclitaxel was shown to decrease tumor growth in a PC-3 prostate cancer mouse xenograft model.1


1.Luo, Y., Shoemaker, A.R., Liu, X., et al.Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivoMol. Cancer Ther.4(6)977-968(2005)

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