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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。
BAY1082439图片
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+;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

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM2.0221 mL10.1104 mL20.2208 mL
5 mM0.4044 mL2.0221 mL4.0442 mL
10 mM0.2022 mL1.0110 mL2.0221 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。