Chemical Name: 2-(4-Morpholinyl)-4H-pyrimido[2,1-a]isoquinolin-4-one
Dual DNA-PK/mTOR inhibitor
Molekulargewicht:
381.32
Reinheit:
>98% by TLC/HPLC (NMR Conforms)
Formulierung:
Off-white solid
CAS Nummer:
[168425-64-7]
Formel:
C16H15N3O2
Anwendungsbeschreibung:
Compound 401 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), IC50s = 0.28 and 5.3 µM, respectively) with selectivity over PI3K, ATM, and ATR.1 Treatment of cells with 401 (10 µM) blocked the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr(389) and Akt Ser(473), respectively) with no direct inhibition of Akt Thr(308) phosphorylation, which is dependent on PI3K.2
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