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WYE-354

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Chemical Structure| 1062169-56-5 同义名 : -
CAS号 : 1062169-56-5
货号 : A121661
分子式 : C24H29N7O5
纯度 : 98%
分子量 : 495.531
MDL号 : MFCD18074514
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

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].
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
实验方案
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
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.