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Description: AT13148 is a novel, potent, orally bioavailable, ATP-competitive, multi-AGC kinase inhibitor with potential anticancer activity. It inhibits Akt1/2/3, p70S6K, PKA, and ROCKI/II with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM respectively. AT13148 caused substantial blockade of AKT, p70S6K, PKA, ROCK, and SGKsubstrate phosphorylation and induced apoptosis in a concentration andtime-dependent manner in cancer cells with clinically relevant geneticdefects in vitro and in vivo. In addition, AT13148 has been revealed to inhibit proliferation with GI50 values of 1.54uM, 1.59uM, 1.82uM, 2.65uM and 3.77uM in MES-SA, BT474, HCT-116, A549 and SK-OV-3 cell lines, respectively.
References:Clin Cancer Res. 2012 Jul 15; 18(14):3912-23.
Related CAS #: 1056901-67-7 (R-isomer); 857532-13-9 (racemic)
Synonym: AT-13148; AT 13148; AT13148; AT13148 hydrochloride; AT13148 HCl
InChi Key: IIRWNGPLJQXWFJ-KRWDZBQOSA-N
InChi Code: InChI=1S/C17H16ClN3O/c18-16-7-5-15(6-8-16)17(22, 11-19)14-3-1-12(2-4-14)13-9-20-21-10-13/h1-10, 22H, 11, 19H2, (H, 20, 21)/t17-/m0/s1
SMILES Code: ClC1=CC=C([C](C2=CC=C(C3=CNN=C3)C=C2)(O)CN)C=C1
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