您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > WYE-354
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
WYE-354
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-354图片
CAS NO:1062169-56-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
WYE-354 是一种 ATP 竞争性的mTOR抑制剂,IC50为 5 nM。WYE-354 也抑制PI3KαPI3KγIC50分别为 1.89 μM 和 7.37 μM。WYE-354 抑制mTORC1mTORC2。WYE-354 在体外能诱导自噬 (autophagy) 激活.
生物活性

WYE-354 is an ATP-competitivemTORinhibitor with anIC50of 5 nM. WYE-354 also inhibitsPI3KαandPI3KγwithIC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits bothmTORC1andmTORC2. WYE-354 inducesautophagyactivation in vitro[3].

IC50& Target[1]

mTOR

5 nM (IC50)

mTORC1

 

mTORC2

 

PI3K alpha

1.89 μM (IC50)

PI3K gamma

7.37 μM (IC50)

Autophagy

 

体外研究
(In Vitro)

In the DELFIA measuring His6-S6K1 T389 phosphorylation, WYE-354 inhibits recombinant mTOR enzyme with an IC50of 5 nM[1]. Cell viability is analyzed by MTS assay. G-415 and TGBC-2TKB cell lines are treated with increasing concentrations of WYE-354 (0.1, 1, 5 and 10 μM) for 24, 48, and 72 hours. WYE-354 significantly reduces cell viability starting at a 1 μM concentration after a 24 hours exposure, in both studied cell lines (P<0.001). A decrease in cell viability is not observed at a dose of 100 nM, except for the TGBC-2TKB cell line after 72 hours of treatment[2].

体内研究
(In Vivo)

The effect of Rapamycin and WYE-354 on tumor growth is evaluated in xenograft GBC tumor models. 2×106or 5×106cells of G-415 or TGBC2TKB, respectively, are xenotransplanted into NOD-SCID mice subcutaneously. When tumors reach an average volume of 100 mm3, the mice are treated either with Rapamycin or WYE354. Rapamycin is administered i.p. at a concentration of 10 mg/kg, daily for 5 days per week for 3 weeks, while WYE-354 is administrated at a daily i.p. dose of 50 mg/kg for 5 days. Mice are sacrificed 30 days after the initiation of the treatments and an autopsy is performed that include removal of the entire tumor area. Mice treated with WYE-354 exhibit 68.6% and 52.4% reduction in average tumor size (P<0.01; P<0.01), as well as 82.9% and 45.5% (P<0.01; ns) reduction in tumor weight, respectively[2].

分子量

495.53

性状

Solid

Formula

C24H29N7O5

CAS 号

1062169-56-5

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 : 6.67 mg/mL(13.46 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0180 mL10.0902 mL20.1804 mL
5 mM0.4036 mL2.0180 mL4.0361 mL
10 mM0.2018 mL1.0090 mL2.0180 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: ≥ 0.67 mg/mL (1.35 mM); Clear solution

    此方案可获得 ≥ 0.67 mg/mL (1.35 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 6.7 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
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 0.67 mg/mL (1.35 mM); Clear solution

    此方案可获得 ≥ 0.67 mg/mL (1.35 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 0.67 mg/mL (1.35 mM); Clear solution

    此方案可获得 ≥ 0.67 mg/mL (1.35 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。