A-674563

Description: A-674563 is a novel and potent Akt1 inhibitor with potential anticancer activity. It binds to Akt with a Ki of 11 nM in cell-free assays, and shows modest potency against PKA and > 30-fold selectivity for Akt1 over PKC. In MiaPaCa-2 cells treated with A-674563 for 48 hour, it slowed the tumor cell proliferation (EC50 = 0.4 um). In STS cells, phosphorylation of GSK3 and MDM2 was prominently reduced by A-674563 treatment. Akt inhibition-induced G2 cells cycle arrest and apoptosis were also observed in A563-treated STS cells.

References: Mol Cancer Ther. 2005 Jun; 4(6):977-86; Cancer Res. 2008 Apr 15; 68(8):2895-903.

Synonym: A674563; A 674563; A-674563

Chemical Name: (S)-1-((5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl)oxy)-3-phenylpropan-2-amine

InChi Key: BPNUQXPIQBZCMR-IBGZPJMESA-N

InChi Code: InChI=1S/C22H22N4O/c1-15-21-11-17(7-8-22(21)26-25-15)18-10-20(13-24-12-18)27-14-19(23)9-16-5-3-2-4-6-16/h2-8, 10-13, 19H, 9, 14, 23H2, 1H3, (H, 25, 26)/t19-/m0/s1

SMILES Code: N[CH](CC1=CC=CC=C1)COC2=CC(C3=CC4=C(NN=C4C)C=C3)=CN=C2