| 产品描述： | 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 |
| 靶点： |
PI3Kα;PI3Kβ;PI3Kδ |
| 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. Cell Viability Assay Cell Line: PC3 and LNCaP cells (PTEN-null human prostate cancer cell lines) Concentration: 0.1, 0.33, 1, 3.3, 10 μM Incubation Time: 72 hours Result: Efectively inhibited cell growth by blocking the G1/S cell cycle transition and by inducing apoptosis. |
| 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. |
| 参考文献： |
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. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.022 ml |
10.11 ml |
20.221 ml |
| 5 mM |
0.404 ml |
2.022 ml |
4.044 ml |
| 10 mM |
0.202 ml |
1.011 ml |
2.022 ml |
| 50 mM |
0.04 ml |
0.202 ml |
0.404 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京