BAY-1082439

PI3Kα、PI3Kβ和PI3Kδ的抑制剂（IC50分别为5、15和1nM）；对PI3Kα、-β和-δ的选择性优于PI3Kγ（IC50=52nM）；以75mg/kg的剂量使用Pten基因敲除小鼠，可降低肿瘤内磷酸化Akt水平并减少去势抵抗性前列腺癌小鼠模型中的肿瘤生长；以180mg/kg的剂量间歇给药可逆转对抗PD-1抗体的耐药性，并在去势Pten基因敲除小鼠的肿瘤微环境中诱导CD8+T细胞克隆扩增和T细胞介导的炎症。An inhibitor of PI3Kα, PI3Kβ, and PI3Kδ (IC50s = 5, 15, and 1 nM, respectively); selective for PI3Kα, -β, and -δ over PI3Kγ (IC50 = 52 nM); decreases intratumoral levels of phosphorylated Akt and reduces tumor growth in a mouse model of castration-resistant prostate cancer using Pten-null mice at 75 mg/kg; intermittent administration 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 at 180 mg/kg.分子式C25H30N6O5分子量494.6COC1=C2C(C3=NCCN3C(NC(C4=C(N=CC=C4)C)=O)=N2)=CC=C1OC[C@H](O)CN5CCOCC5