BAY1082439

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BAY1082439

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1375469-38-7

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

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。

生物活性

BAY1082439 is an orally bioavailable, selectivePI3Kα/β/δinhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibitingPten-null prostatecancergrowth^[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 IC₅₀ratio 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].

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 preventingPten-null prostate cancer progression^[2].

Animal Model:	Pten conditional knockout mouse model (Pb-Cre⁺;Pten^L/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

性状

Solid

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。