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Overview
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Background
AT13148 is a novel, oral and ATP-competitive inhibitor of multi-AGC Kinase with IC50 values of 38nM, 8nM, 3nM, 63nM and 4nM for AKT, p70S6 kinase, PKA, SGK and Rho kinase, respectively [1].In vitro studies, AT13148 has been reported to inhibit activity of AGC kinases which including AKT, p70S6 kinase, PKA, SGK and Rho kinase with the IC50 values of 38nM, 8nM, 3nM, 63nM and 4nM, respectively. In addition, AT13148 has been revealed to inhibit proliferation with GI50 values of 1.54μM, 1.59μM, 1.82μM, 2.65μM and 3.77μM in MES-SA, BT474, HCT-116, A549 and SK-OV-3 cell lines, respectively.In vivo studies, AT13148 has shown the antitumor activity in multiple human tumor xenograft models including PTEN-deficient MES-SA human uterine sarcoma, HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts [1].
[1] Yap TA1, Walton MI, Grimshaw KM, Te Poele RH, Eve PD, Valenti MR, de Haven Brandon AK, Martins V, Zetterlund A, Heaton SP, Heinzmann K, Jones PS, Feltell RE, Reule M, Woodhead SJ, Davies TG, Lyons JF, Raynaud FI, Eccles SA, Workman P, Thompson NT, Garrett MD. AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity. Clin Cancer Res. 2012 Jul 15;18(14):3912-23.
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- Properties
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