85-4471-17　A-674563 500ug　349624

特徴

• Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBalpha, beta, gamma) modulate cell proliferation, metabolism, and survival, as well as angiogenesis. A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki =11nM for Akt1). 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. A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4uM.1 In vivo, 40mg/kg/day A-674563 in combination with 15mg/kg/day paclitaxel was shown to decrease tumor growth in a PC-3 prostate cancer mouse xenograft model.
• Molecular Formula:C22H22N4O
• Solubility:~0.5mg/ml in a 1:1 solution of DMF:PBS (pH 7.2); ~10mg/ml in EtOH; ~15mg/ml inDMSO; ~20mg/ml in DMF
• Molecular Weight:358.4
• Lambda max:245, 299nm
• Storage and Stability:Lyophilized powder may be stored at -20°C. Reconstitute with ethanol, DMSO or DMF. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.