化合物BAY1082439 T14511

Product Introduction
Bioactivity


英文名: BAY1082439

描述: 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。

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : Slightly soluble


关键字: PTEN | BAY 1082439 | inhibit | cancer | oral | Inhibitor | BAY-1082439 | forms | Phosphoinositide 3-kinase | PI3K | Apoptosis | BAY1082439 | mutated | PIK3CA | prostate

相关产品: Notoginsenoside R1 | Methotrexate | Isatin | (Rac)-Antineoplaston A10 | BIBR 1532 | Delanzomib | Lysophosphatidylcholines | BAY 11-7082 | Triglycidyl isocyanurate | Isolongifolene

相关库: Drug Repurposing Compound Library | PI3K-AKT-mTOR Compound Library | Anti-Prostate Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Reprogramming Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途