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. CAS Number: 552325-73-2 Molecular Formula: C22H22N4O Solubility: ~0.5mg/ml in a 1:1 solution of DMF:PBS (pH 7.2), ~10mg/ml in EtOH, ~15mg/ml in DMSO, ~20mg/ml in DMF Molecular Weight: 358.4 Lambda max: 245, 299nm Storage and Stability: Lyophilized powder may be stored at -20C. Reconstitute with ethanol, DMSO or DMF. Aliquot to avoid repeated freezing and thawing. Store at -20C. 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.
Molecular Weight:
358.4
Purity:
Highly Purified (~95%)
Form:
Supplied as a crystalline solid.
CAS Number:
[552325-73-2]
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