AZD3147 is novel urea containing morpholinopyrimidine compound and is an extremely potent and selective dual inhibitor of mTORC1 (rapamycin sensitive complex) and mTORC2 (rapamycin insensitive complex). It has physicochemical and pharmacokinetic properties suitable for development as a potential clinical candidate. mTOR enzyme IC50 = 0.0015μM, mTOR cells IC50 = 0.006μM, PI3Kα,β,δ,γ enzyme IC50 = 0.92, 5.5, 9.4 and 6.3 μM respectively.
Systematic Name: (S)-1-(4-(4-(1-(cyclopropylsulfonyl)cyclopropyl)-6-(3-methylmorpholino)pyrimidin-2-yl)phenyl)-3-(2-hydroxyethyl)thiourea
Chemical Formula: C24H31N5O4S2
Molecular Weight: 517.66
Reference: Pike, Kurt G., et al. "Discovery of AZD3147: A potent, selective dual inhibitor of mTORC1 and mTORC2." Journal of Medicinal Chemistry 58.5 (2015): 2326-2349.
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Tags: RGNCY-0025, AZD3147, Morpholinopyrimidine, mTORC1, mTORC2, TORC, TOR