BAY1082439

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BAY1082439  纯度: 99.46%

BAY1082439 是一种具有口服活性的，选择性 PI3Kα/β/δ 抑制剂。BAY1082439 也能抑制 PIK3CA 的突变形式，BAY1082439 对抑制 Pten 丢失的前列腺癌的生长有很强的作用。

BAY1082439

BAY1082439 Chemical Structure

CAS No. : 1375469-38-7

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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[1][2].

IC50 & Target[1]

PI3Kα

 

PI3Kβ

 

PI3Kδ

 

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

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
(In Vivo)

BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pten conditional knockout mouse model (Pb-Cre+;PtenL/L, CP model)[2]
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.

Clinical Trial

分子量

494.54

Formula

C25H30N6O5
CAS 号

1375469-38-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (10.11 mM; ultrasonic and adjust pH to 5 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0221 mL 10.1104 mL 20.2208 mL
5 mM 0.4044 mL 2.0221 mL 4.0442 mL
10 mM 0.2022 mL 1.0110 mL 2.0221 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

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