化合物WYE354 T6731

Product Introduction
Bioactivity


英文名: WYE-354

描述: WYE-354 是一种 ATP 竞争性的mTOR 抑制剂，IC50为 5 nM。它抑制PI3Kα和PI3Kγ，IC50分别为 1.89 μM 和 7.37 μM，也抑制mTORC1和mTORC2。它在体外能诱导自噬激活。

细胞实验: Tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, DU145, A498, and HCT116, are plated in 96-well plates at 1000 to 3000 cells per well for 24 hours, treated with DMSO or varying concentrations of WYE-354(0–50 μM, dissolved in DMSO) for72 hours.

激酶实验: The assays were incubated at room temperature for 2 hours. In 96-well plates (25 μL) contains 6 nM Flag-TOR(3.5) (estimated 5-10% purity), 1 μM His6-S6K and 100 μM ATP.For inhibitor versus ATP matrix competition, mTOR kinase reactions are carried out with varying concentrations of ATP (0, 25, 50 100, 200, 400 and 800 μM) in combination with varying concentrations of inhibitor.The assays are performed and detected by DELFIA employing the Euphospho-p70S6K T389 antibody.

动物实验: Nude mice (BALB/c, nu/nu, female) bearing PC3 mM2 xenograft were intraperitoneally injected with WYE-354（50 mg/kg）dissolved in 5% ethanol, 5% polysorbate 80, 5% PEG-400.

体外活性: In HEK293 cells, WYE-354 (0.2 μM–5 μM) effectively inhibits both mTORC1 and mTORC2. In U87 mg and MDA361 cells, WYE-354 (0.3 μM–10 μM) significantly blocks mTOR signaling and Akt activation. In tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, A498, and HCT116, WYE-354 effectively inhibits proliferation with IC50 values ranging from 0.28 μM to 2.3 μM. In endothelial HUVEC cells, WYE-354 also inhibits both mTORC1 and mTORC2 signaling with IC50 values ranging from 10 nM to 1 μM, as revealed by dephosphorylation of S6 ribosomal protein and Akt, respectively. The apoptosis induced by WYE-354 is accompanied by G1 cell cycle arrest and caspases activation.WYE-354 (10 nM–1 μM) activates mitogen-activated protein kinase (MAPK) signaling, which may be due to its inhibition of mTORC1.

体内活性: WYE-354 (50 mg/kg) 在PTEN-null PC3 mM2肿瘤的小鼠异种移植模型中，强效抑制mTOR信号传导和肿瘤生长。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 92 mg/mL (185.7 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | Apoptosis | WYE354 | WYE 354 | Inhibitor | WYE-354 | Autophagy | Mammalian target of Rapamycin | mTOR

相关产品: Y-27632 | Abacavir | FMAU | EPZ004777 | PNU-74654 | Sulforaphane | Ginkgolide B | Topotecan hydrochloride | T-1101 tosylate | SB 415286

相关库: Anti-Breast Cancer Compound Library | Pyroptosis Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Highly Selective Inhibitor Library | Autophagy Compound Library | Stem Cell Differentiation Compound Library | Glycolysis Compound Library

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