BAY1082439 是一种具有口服活性的，选择性PI3Kα/β/δ抑制剂。它也能抑制 PIK3CA 的突变形式，它对抑制PTEN丢失的前列腺癌的生长有很强的作用。
产品描述
BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth[1][2] and it is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA.
体外活性
BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells[2]. 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[1].
体内活性
BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression[2].
Cas No.
1375469-38-7
分子式
C25H30N6O5
分子量
494.54
别名
N-[8-[[(2R)-2-羟基-3-(吗啉-4-基)丙基]氧基]-7-甲氧基-2,3-二氢咪唑并[1,2-C]喹唑啉-5-基]-2-甲基吡啶-3-甲酰胺;BAY1082439
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
