CAS No. : 1056901-62-2

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000296
Molecular Formula:C₁₇H₁₆ClN₃O
Molecular Weight:313.78
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Appearance:white solid powder
Purity: > 98%
Cat No:I000296
Cas No:1056901-62-2

AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity; AKT, p70S6K, PKA, ROCK, and SGK inhibitor.
IC50 value:
Target: AGC kinase
AT13148 caused substantial blockade of AKT, p70S6K, PKA, ROCK, and SGK substrate phosphorylation and induced apoptosis in a concentration and time-dependent manner in cancer cells with clinically relevant genetic defects in vitro and in vivo. Antitumor efficacy in HER2-positive, PIK3CA-mutant BT474 breast, PTEN-deficient PC3 human prostate cancer, and PTEN-deficient MES-SA uterine tumor xenografts was shown. We show for the first time that induction of AKT phosphorylation at serine 473 by AT13148, as reported for other ATP-competitive inhibitors of AKT, is not a therapeutically relevant reactivation step. Gene expression studies showed that AT13148 has a predominant effect on apoptosis genes, whereas the selective AKT inhibitor CCT128930 modulates cell-cycle genes. Induction of upstream regulators including IRS2 and PIK3IP1 as a result of compensatory feedback loops was observed.

1:AT13148, a first-in-class multi-AGC kinase inhibitor, potently inhibits gastric cancer cells both in vitro and in vivo. Xi Y, Niu J, Shen Y, Li D, Peng X, Wu X.Biochem Biophys Res Commun. 2016 Sep 9;478(1):330-6. doi: 10.1016/j.bbrc.2016.01.167. Epub 2016 Jan 30. PMID: 26828267
2:Role of the anti-glioma drug AT13148 in the inhibition of Notch signaling pathway. Min W, Li Y, Zhang Y, Dai D, Cao Y, Yue Z, Liu J.Gene. 2015 Nov 15;573(1):153-9. doi: 10.1016/j.gene.2015.07.033. Epub 2015 Jul 15. PMID: 26187072
3:AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity. Yap TA, 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.Clin Cancer Res. 2012 Jul 15;18(14):3912-23. doi: 10.1158/1078-0432.CCR-11-3313. Epub 2012 Jul 10. PMID: 22781553 Free Article
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