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A-674563 A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC. Synonyms: A674563; A 674563; Benzeneethanamine, α-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-, (αS)-; (α S) -α - [ [ [5- (3-Methyl-1H-indazol-5-yl) -3-pyridinyl] oxy] methyl] benzeneethanamine; (S)-1-((5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl)oxy)-3-phenylpropan-2-amine. Grades: >98%. CAS No. 552325-73-2. Molecular formula: C22H22N4O. Mole weight: 358.44. BOC Sciences
A-674563 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. Group: Biochemicals. Alternative Names: (αS-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]- benzeneethanamine). Grades: Highly Purified. CAS No. 552325-73-2. Pack Sizes: 500ug, 1mg, 5mg, 10mg. Molecular Formula: C22H22N4O. US Biological Life Sciences. USBiological 9
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