A-674563

Biological Activity

A-674563 is a potent selective Akt1 (Protein Kinase B) inhibitor (IC50 = 14 nM). A-674563 also shows inhibitory activity against PKA and Cdk2 (IC50’s: PKA = 16 nM; Cdk2 = 46 nM). A-674563 has been shown to have a significant effect on depolarization of purkinje fiber in an in vitro assay, and severe CV toxicity (e.g. hypotension) in vivo. The X-ray structure of A-674563 bound to protein kinase A, which exhibits 80% homology with Akt in the kinase domain, suggested the phenyl group is not tightly bound in the ligand-protein complex. The Akt inhibitor A-674563 displayed proliferation of tumor cells (EC50: 0.4 μM). When given in combination, A-674563 enhanced the efficacy of paclitaxel in a PC-3 xenograft model.For the detailed information of A-674563, the solubility of A-674563 in water, the solubility of A-674563 in DMSO, the solubility of A-674563 in PBS buffer, the animal experiment (test) of A-674563, the cell expriment (test) of A-674563, the in vivo, in vitro and clinical trial test of A-674563, the EC50, IC50,and Affinity of A-674563, Please contact DC Chemicals.

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.