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BAY1125976
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。
BAY1125976图片
CAS NO:1402608-02-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
BAY1125976 是Akt1/Akt2选择性的变构抑制剂;在10 μM ATP 时抑制 Akt1 和 Akt2 活性的IC50值分别为 5.2 nM 和 18 nM。
生物活性

BAY1125976 is a selective allostericAkt1/Akt2inhibitor; inhibitsAkt1andAkt2activity withIC50values of 5.2 nM and 18 nM at 10 μM ATP, respectively.

IC50& Target

Akt1

5.2 nM (IC50, at 10 μM ATP)

Akt2

18 nM (IC50, at 10 μM ATP)

Akt3

427 nM (IC50, at 10 μM ATP)

体外研究
(In Vitro)

BAY 1125976 is equally potent against Akt1 (IC50=5.2 nM at 10 μM ATP and 44 nM at 2 mM ATP) and Akt2 (IC50=18 nM at 10 μM ATP and 36 nM at 2 mM ATP) isoforms and up to 86 fold less potent against Akt3 (IC50=427 nM at 10 μM ATP). It inhibits the Akt1 and Akt2 by binding into an allosteric binding pocket formed by kinase and PH domain. It inhibits cell proliferation in a broad panel of human cancer cell lines, particularly in breast and prostate cancer cell lines expressing estrogen or androgen receptors. It effectively blocks Akt signaling by inhibiting the phosphorylation of Akt and the downstream effectors, including eukaryotic translation initiation factor 4E binding protein 1 (4E-BP1), glycogen synthase kinase 3 beta (GSK3s), proline-rich Akt substrate 40 kDa (PRAS40), S6 ribosomal protein (S6RP), and 70 kDa ribosomal protein S6 kinase 1 (70S6K)[1].

体内研究
(In Vivo)

BAY 1125976 targets tumors displaying activation of the PI3K/Akt/mTOR pathway. BAY 1125976 exhibits strongin vivoefficacy in both cell line and patient-derived xenograft models such as the KPL4 breast cancer model (PIK3CAH1074Rmutant), the MCF7 and HBCx-2 breast cancer models, and the AktE17Kmutant driven prostate cancer (LAPC-4) and anal cancer (AXF 984) models[1].

Clinical Trial
分子量

383.45

性状

Solid

Formula

C23H21N5O

CAS 号

1402608-02-9

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 : 25 mg/mL(65.20 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6079 mL13.0395 mL26.0790 mL
5 mM0.5216 mL2.6079 mL5.2158 mL
10 mM0.2608 mL1.3040 mL2.6079 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.52 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。