WYE-354 | mTOR Inhibitor | AmBeed-信号通路专用抑制剂

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WYE-354 98%

货号：A121661

WYE-354是一种 ATP 竞争性的哺乳动物雷帕霉素靶蛋白 (mTOR) 抑制剂，IC50 为 5 nM。它还抑制 PI3Kα 和 PI3Kγ，IC50 值分别为 1.89 μM 和 7.37 μM。

WYE-354 化学结构
CAS号：1062169-56-5

WYE-354 3D分子结构
CAS号：1062169-56-5

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WYE-354 纯度/质量文件产品仅供科研

货号：A121661 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

mTOR 亚型比较

产品名称	mTOR ↓ ↑	mTORC1 ↓ ↑	mTORC2 ↓ ↑	其他靶点	纯度
AZD-8055	++++ mTOR (full length), IC50: 0.8 nM mTOR (truncated), IC50: 0.13 nM				99%+
Gedatolisib	++++ mTOR, IC50: 1.6 nM				98%
GSK1059615	++ mTOR, IC50: 12 nM				98%
Vistusertib	+++ mTOR, IC50: 2.8 nM				99%+
Torin 1	+++ mTOR, IC50: 4.32 nM	+++ mTORC1, IC50: 2 nM	++ mTORC2, IC50: 10 nM	DNA-PK	99%+
Dactolisib	+++ mTOR (p70S6K), IC50: 6 nM				98+%
PI-103	+ mTOR, IC50: 30 nM				99%+
WAY-600	++ mTOR, IC50: 9 nM				99%
Voxtalisib	+ mTOR, IC50: 157 nM				99%+
PF-04691502	++ mTOR, Ki: 16 nM				98+%
Onatasertib	++ mTOR, IC50: 16 nM			DNA-PK	99%+
Chrysophanol	✔			EGFR	98%
Samotolisib	✔			DNA-PK	99%+
Torkinib	+++ mTOR, IC50: 8 nM			PDGFR,DNA-PK	99%+
Everolimus					99%+
WYE-354	+++ mTOR, IC50: 5 nM				98%
Tacrolimus	✔				98%
PP121	++ mTOR, IC50: 13 nM			PDGFR,VEGFR	99%+
Torin 2	++++ mTOR, IC50: 0.25 nM			DNA-PK	99%+
Rapamycin	++++ mTOR, IC50: ~0.1 nM				98%
GDC-0349	+++ mTOR, Ki: 3.8 nM				98%
XL388	++ mTOR, IC50: 9.9 nM	+++ mTORC1, IC50: 8 nM	+ mTORC2, IC50: 166 nM		99%+
WYE-687	+++ mTOR, IC50: 7 nM				98+%
Apitolisib	+ mTOR, Ki app: 17 nM				98%+
WYE-132	++++ mTOR, IC50: 0.19 nM				99%+
Sapanisertib	++++ mTOR, Ki: 1.4 nM				99%+
BGT226 maleate	✔				99%+
ETP-46464	++++ mTOR, IC50: 0.6 nM			DNA-PK	98%
PI3K-IN-1	+ mTOR, IC50: 157 nM				98+%
Zotarolimus	+++ FKBP-12, IC50: 2.8 nM				99+%
OSI-027	+++ mTOR, IC50: 4 nM	+ mTORC1, IC50: 22 nM	+ mTORC2, IC50: 65 nM		99%+
Ridaforolimus	++++ mTOR, IC50: 0.2 nM				99%+
Temsirolimus	+ mTOR, IC50: 1.76 μM				99%
CZ415	++ mTOR, pIC50: 8.07				99%+
SF2523	+ mTOR, IC50: 280 nM			DNA-PK	99%+
KU-0063794		++ mTORC1, IC50: ~10 nM	++ mTORC2, IC50: ~10 nM		99%+
Omipalisib		++++ mTORC1, Ki: 0.18 nM	++++ mTORC2, Ki: 0.3 nM		99%+
Palomid 529		✔			99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

WYE-354 生物活性

靶点

mTOR

mTOR, IC50:5 nM

描述

The mammalian target of rapamycin (mTOR) is centrally involved in cell growth, metabolism, and angiogenesis^[3]. WYE-354 is an ATP-competitive mTOR inhibitor with an IC₅₀ of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC₅₀s of 1.89 μM and 7.37 μM, respectively ^[3]. In vitro assays showed WYE-354 significantly reduced cell viability, migration and invasion and phospho-P70S6K expression in GBC cells^[4]. When injected into tumor-bearing mice, WYE-354 inhibited mTORC1 and mTORC2 and displayed robust antitumor activity in PTEN-null tumors ^[3]. Mice harboring subcutaneous gallbladder tumors, treated with WYE-354, exhibited a significant reduction in tumor mass. A short-term treatment with a higher dose of WYE-354 decreased the tumor size by 68.6% and 52.4% , in mice harboring G-415 or TGBC-2TKB tumors, respectively, compared to the control group^[4].

WYE-354 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HEK293 cells		Function assay		Inhibition of flag-tagged truncated human mTOR (1360-2549) expressed in HEK293 cells by DELFIA assay, IC50=0.0043 μM	19645448
LNCAP cells		Cytotoxicity assay	3 days	Cytotoxicity against human LNCAP cells after 3 days by MTS assay, IC50=0.355 μM	19645448

WYE-354 参考文献

[1]Dormond-Meuwly A, Roulin D, et al. The inhibition of MAPK potentiates the anti-angiogenic efficacy of mTOR inhibitors. Biochem Biophys Res Commun. 2011 Apr 22;407(4):714-9.

[2]Yu K, Toral-Barza L, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009 Aug 1;69(15):6232-40.

[3]Yu K, Toral-Barza L, Shi C, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009;69(15):6232–6240.

[4]Weber H, Leal P, Stein S, et al. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice. Oncotarget. 2015;6(31):31877–31888.

WYE-354 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.09mL

2.02mL

1.01mL

20.18mL

4.04mL

2.02mL

WYE-354 技术信息

CAS号	1062169-56-5
分子式	C₂₄H₂₉N₇O₅
分子量	495.531

别名
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 5 mg/mL(10.09 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

4% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

WYE-354 98%

WYE-354 纯度/质量文件产品仅供科研

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WYE-354 98%

WYE-354 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

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WYE-354 生物活性

WYE-354 细胞研究

WYE-354 参考文献

WYE-354 实验方案

WYE-354 技术信息

最近浏览的产品

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