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Description: AZD8186 (also known as AZD) is a novel, potent and selective inhibitor of PI3Kbeta (phosphatidylinositol 3-kinase beta) with potential anticancer activity. It inhibits PI3Kbeta and PI3Kdelta with IC50 of 4 nM and 12 nM, respectively, and showed high selectivity for PI3Kbeta and PI3Kdelta over PI3Kgamma (IC50=675 nM). AZD8186 exhibits significant anti-tumour activity inPTEN-deficient preclinical models, particularly when combined withanti-androgens or the dual mTORC1/2 inhibitor vistusertib (AZD2014). AZD8186 has a potential for treatment of PTEN-deficient tumors.
References:J Med Chem. 2015 Jan 22; 58(2):943-62.
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