552325-73-2

A-674563

552325-73-2

编号ABP000415 化学名称A-674563 英文名称 A-674563 分子式C22H23ClN4O 分子量394.897 纯度 >99%

化学名称 : A-674563

CAS : 552325-73-2

英文名称: A-674563

英文同义词: (S)-1-(5-(3-Methyl-1H-indazol-5-yl)pyridin-3-yloxy)-3-phenylpropan-2-amine hydrochloride

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

A-674563 is a potent selective protein kinase B/Akt inhibitor with an IC50 of 14 nM. A-674563 also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively. While promising efficacy was observed in vivo, A-674563 indicated significantly effects on depolarization of purkinje fiber in an in vitro assay and severe CV toxicity (e.g. hypotension) in vivo. An X-ray structure of A-674563 bound to protein kinase A, which has 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 with an EC50 of 0.4 μM. When given in combination, A-674563 enhanced the efficacy of paclitaxel in a PC-3 xenograft model.[1][2]

参考文献

[1] Luo Y et al. Mol Cancer Ther. 2005 Jun;4(6):977-86.

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