WYE-354

SKU: orb1300518

Description

WYE-354 is a potent, selective, and ATP-competitive mTOR inhibitor with an IC50 of 5 nM. It effectively suppresses mTORC2-mediated P-AKT(S473) and mTORC1-mediated P-S6K(T389) signaling, demonstrating high selectivity over PI3K isoforms. This inhibitor is a valuable tool for investigating mTOR pathway biology in both cellular and in vivo cancer research models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1062169-56-5
• MW: 495.53
• Purity: 99.61% (May vary between batches)
• Formula: C₂₄H₂₉N₇O₅
• SMILES: COC(=O)Nc1ccc(cc1)-c1nc(N2CCOCC2)c2cnn(C3CCN(CC3)C(=O)OC)c2n1
• Target: Autophagy,mTOR,PI3K,Apoptosis
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:92 mg/mL (185.66 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (2.02 mM)

Bioactivity

• Target IC50:
  PI3Kγ:7.37 μM|mTOR:5 nM|PI3Kα:1.89 μM
• In Vivo:
  WYE-354 (50 mg/kg) potently inhibits mTOR signaling and tumor growth In a mice xenograft model of PTEN-null PC3 mM2 tumor.
• In Vitro:
  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.
• Cell Research:
  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.
• Animal Research:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, Apoptosis, inhibit, mTOR, Inhibitor, Mammalian target of Rapamycin, WYE 354, WYE-354, PI3Kα, WYE354, PI3Kγ

Compound Identifiers

PubChem CID

44219749