Formulation: A solid
Formal Name: N-[2,3-dihydro-8-[(2R)-2-hydroxy-3-(4-morpholinyl)propoxy]-7-methoxyimidazo[1,2-c]quinazolin-5-yl]-2-methyl-3-pyridinecarboxamide
Purity: ≥98%
Formula Markup: C25H30N6O5
Formula Weight: 494,6
Shelf life (days): 730
CAS Number: 1375469-38-7
Notes: BAY-1082439 is an inhibitor of PI3Kα, PI3Kβ, and PI3Kδ (IC50s = 5, 15, and 1 nM, respectively).{68014} It is selective for PI3Kα, -β, and -δ over PI3Kγ (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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