A-674563 hydrochloride

An Akt inhibitor

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库存: 现货

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2mg

￥1025.00

820.00

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5mg

￥1775.00

1420.00

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10mg

￥2800.00

2240.00

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50mg

￥8350.00

6680.00

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100mg

￥12462.00

9970.00

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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 (K_i = 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)