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Biological Activity:
Potent and cell permeable PI3K inhibitor, with IC50 values (nM) of 11, 350, 18, and 58 for p110 α, β, γ and δ isoforms, low mTOR activity.
References: online 1, 2, 3, 4, 5
JS Chen et al. Characterization of structurally distinct, isoform-selective phosphoinositide 3′-kinase inhibitors in combination with radiation in the treatment of glioblastoma. Mol. Cancer Ther. 2008, 7, 841-850.
ZA Knight et al. A Pharmacological Map of the PI3-K Family Defines a Role for p110α in Insulin Signaling. Cell 2006, 125, 733–747.
C Chaussade et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007, 404(3), 449–458.
S Kim et al. Insulin-like growth factor-1 regulates platelet activation through PI3-Kα isoform. Blood, 2007, 110(13), 4206-4213.
Chemical Name: N-(7,8-Dimethoxy-2,3-dihydro-imidazo[1,2-c]quinazolin-5-yl)-nicotinamide
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