产品
编 号:F142714
分子式:C25H30N6O5
分子量:494.54
产品类型
结构图
CAS No: 1375469-38-7
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产品详情
生物活性:
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
体内研究:
BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression.Animal Model: Pten conditional knockout mouse model (Pb-Cre+;PtenL/L, CP model)
Dosage:75 mg/kg
Administration:P.o.; daily for 4 weeks
Result:Significantly decreased tumor size and P-AKT staining, nearly normal luminal architecture, and a significant reduction of Ki67-positive cells. Significantly inhibit the human prostate cancer growth.
体外研究:
BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 has an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase.BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells.