BAY-1082439

BAY-1082439

CAT N°: 35456
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From 117.00 99.45

BAY-1082439 is an inhibitor of PI3K?, PI3K?, and PI3K? (IC50s = 5, 15, and 1 nM, respectively).{68014} It is selective for PI3K?, -?, and -? over PI3K? (IC50 = 52 nM). BAY-1082439 selectively inhibits proliferation of PTEN-null LNCaP and PC3 prostate cancer cells over wild-type PTEN isogenic PC3 cells. BAY-1082439 (75 mg/kg) decreases intratumoral levels of phosphorylated Akt and reduces tumor growth in a mouse model of castration-resistant prostate cancer using castrated Pten conditional knockout mice (Pten-null mice). Intermittent administration of BAY-1082439 (180 mg/kg) reverses resistance to an anti-PD-1 antibody and induces CD8+ T cell clonal expansion and T cell-mediated inflammation in the tumor microenvironment in castrated Pten-null mice.{68015}

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