AT7867 - CAS 857531-00-1
Catalog number: 857531-00-1
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H20ClN3
Molecular Weight:
337.85
COA:
Inquire
Targets:
Akt
Description:
AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family.
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Purity:
>98%
Synonyms:
AMG-706
MSDS:
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1.AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth.
Grimshaw KM1, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD. Mol Cancer Ther. 2010 May;9(5):1100-10. doi: 10.1158/1535-7163.MCT-09-0986. Epub 2010 Apr 27.
The serine/threonine kinase AKT plays a pivotal role in signal transduction events involved in malignant transformation and chemoresistance and is an attractive target for the development of cancer therapeutics. Fragment-based lead discovery, combined with structure-based drug design, has recently identified AT7867 as a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A. This ATP-competitive small molecule potently inhibits both AKT and p70S6K activity at the cellular level, as measured by inhibition of GSK3beta and S6 ribosomal protein phosphorylation, and also causes growth inhibition in a range of human cancer cell lines as a single agent. Induction of apoptosis was detected by multiple methods in tumor cells following AT7867 treatment. Administration of AT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) to athymic mice implanted with the PTEN-deficient U87MG human glioblastoma xenograft model caused inhibition of phosphorylation of downstream substrates of both AKT and p70S6K and induction of apoptosis, confirming the observations made in vitro.
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CAS 857531-00-1 AT7867

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