Catalog No.: PC-20556Not For Human Use, Lab Use Only.
AT13148 (AT 13148) is a potent, ATP-competitive and orally active multi-AGC kinase inhibitor with IC50 vaules of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
AT13148 (AT 13148) is a potent, ATP-competitive and orally active multi-AGC kinase inhibitor with IC50 vaules of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. AT13148 potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines. AT13148 dramatically suppresses activation of multiple AGC kinases, including Akt (at p-Thr-308), p70S6 kinase (p70S6K), glycogen synthase kinase 3β (GSK-3β) and p90 ribosomal S6 kinase (RSK) in gastric cancer cells. AT13148 (40 and 50 mg/kg p.o.) inhibits phosphorylation of the AKT substrates GSK3β, tuberin, and the p70S6K target S6RP are also observed in PTEN-deficient MES-SA human uterine tumor xenografts. AT13148 significantly inhibits HGC27 xenograft tumor growth in nude mice.
Physicochemical Properties
M.Wt
313.79
Formula
C17H16ClN3O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
O[C@@](C1=CC=C(Cl)C=C1)(CN)C2=CC=C(C3=CNN=C3)C=C2
References
1. Yap TA, et al. Clin Cancer Res. 2012 Jul 15;18(14):3912-23.
2. Xi Y, et al. Biochem Biophys Res Commun. 2016 Sep 9;478(1):330-6.
