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WYE-132
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。
WYE-132图片
CAS NO:1144068-46-1
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

产品名称
WYE-125132
产品介绍
WYE-132 (WYE-125132) 是一种高度有效的 ATP 竞争性和特异性mTOR激酶抑制剂 (IC50为 0.19±0.07 nM)。WYE-132 (WYE-125132) 抑制mTORC1mTORC2
生物活性

WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specificmTORkinase inhibitor (IC50: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibitsmTORC1andmTORC2.

IC50& Target

mTORC1

 

mTORC2

 

mTOR

0.19 nM (IC50)

PI3Kα

1.179 μM (IC50)

PI3Kδ

2.38 μM (IC50)

hSMG1

1.25 μM (IC50)

体外研究
(In Vitro)

WYE-132 (WYE-125132) potently inhibits recombinant mTOR via an ATP-competitive mechanism. WYE-132 is a potent antiproliferative agent against a panel of cancer cell lines with IC50values generally in the nanomolar range. In the typical 3-day dose-response studies, WYE-132 exhibits a more profound antiproliferative activity than CCI-779 in MDA361 and other cells, as shown by the sharper inhibition at doses up to 10 μM. Fluorescence-activated cell sorting (FACS) analysis of inhibitor-treated (1 μM, 24 hours) MDA468, PC3MM2, U87MG, A549, and HCT116 cells indicates that WYE-132 elicits a more profound increase in G1-phase and a reduction in S-phase cells than CCI-779. The WYE-132-induced cell death is evident at 10 and 30 nM (6.2% and 13%, respectively) and is dose dependent, reaching 47% at 1 μM and 59% at 3 μM[1].

体内研究
(In Vivo)

A single i.v. administration of 50 mg/kg WYE-132 (WYE-125132) into tumor-bearing mice leads to suppression of P-S6K(T389) and P-AKT(S473) for at least 8 hours in PC3MM2, MDA361, HCT116, and HT29 tumors, whereas the steady-state level of P-AKT(T308) is not significantly reduced, indicating that the antitumor efficacy of WYE-132 under such dosing regimens reflects the suppression of mTOR rather than PI3K. Oral administration of WYE-132 causes dose-dependent tumor growth delay in the PI3K/mTOR- and HER2-hyperactive MDA361 tumors with significant antitumor activity at 5 mg/kg, which correlates with a suppression P-S6 and P-AKT(S473) but not P-AKT(T308). An optimal dose of 50 mg/kg WYE-132 induces a substantial regression of large MDA361 tumors. WYE-132 also causes a potent and substantial tumor growth delay in the PTEN-null U87MG glioma[1].

分子量

519.60

性状

Solid

Formula

C27H33N7O4

CAS 号

1144068-46-1

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(48.11 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9246 mL9.6228 mL19.2456 mL
5 mM0.3849 mL1.9246 mL3.8491 mL
10 mM0.1925 mL0.9623 mL1.9246 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 (4.81 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.81 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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。