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Cat. No. Name Size Price Add Cart
KI0536AT13148QuoteQuote

Chemical Characteristic

Product NameAT13148
CAS No.1056901-62-2
Molecular Weight 313.78
FormulaC17H16ClN3O
Chemical Name(+)-(S)-2-Amino-1-(4-chlorophenyl)-1-[4-(1H-pyrazol-4-yl)phenyl]ethanol
Smiles[C@](CN)(c1ccc(cc1)c1cn[nH]c1)(c1ccc(cc1)Cl)O
Chemical Structure

Biological activities

AT13148 is an oral ATP-competitive multi-AGC kinase inhibitor. The IC50 values of AT13148 are all less than 10 nM against p70S6K, PKA, ROCKI, and ROCKII. The IC50 values of AT13148 are 38, 402, and 50 nM against AKT1, AKT2, and AKT3, respectively. For the related AGC kinases RSK1 and SGK3, the IC50 values of AT13148 are 85 and 63 nM, respectively. In contrast, IC50 values of AT13148 for the non-AGC kinases CHK2 and Aurora B are both greater than 800 nM. In vitro, AT13148 potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a panel of cancer cell lines. AT13148 treatment also shows clear inhibition of phos-phorylation on direct substrates of the AGC kinases PKA, ROCK , and SGK in U87MG cells. AT13148 treatment inhibits AKT and p70S6K signaling in PTEN-deficient MES-SA cells. In HER2-positive, PIK3CA-mutant BT474 breast, PTEN-deficient PC3 human prostate cancer, and PTEN-deficient MES-SA uterine tumor xenografts, AT13148 treatment (40 or 50 mg/kg) has antitumor efficacy.[1]

Protocols

In vitro: AT13148 is dissolved in DMSO.[1]

References

[1] Yap TA, et al. AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity. Clin Cancer Res. 2012, 18(14): 3912-3923.

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