BAY1082439 |
| Catalog No.GC62164 |
BAY1082439는 경구 생체이용 가능한 선택적 PI3Kα/β/δ 억제제입니다. BAY1082439는 또한 PIK3CA의 돌연변이 형태를 억제합니다. BAY1082439는 Pten-null 전립선암 성장을 억제하는 데 매우 효과적입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1375469-38-7
Sample solution is provided at 25 µL, 10mM.
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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[1][2].
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[1].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 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression[2].
[1]. Ningshu Liu, et al. Abstract 2799: BAY 1082439, a highly selective and balanced PI3Kα/β inhibitor demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN. Abstract nr 2799. doi:1538-7445.AM2012-2799.
[2]. Yongkang Zou, et al. Co-Targeting the Cell Intrinsic and Microenvironment Pathways of Prostate Cancer by PI3Kα/β/δ inhibitor BAY1082439. Mol Cancer Ther. 2018 Oct;17(10):2091-2099.
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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