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WYE-354

Catalog No. T6731 CAS 1062169-56-5

WYE-354(IC50=5 nM) is an effective, selective and ATP-competitive mTOR inhibitor. It blocks mTORC2/P-AKT(S473) and mTORC1/P-S6K(T389), not P-AKT(T308). The selectivity for mTOR is higher than PI3Kα (<100-fold) and PI3Kγ (<500-fold).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

WYE-354, CAS 1062169-56-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 158.00
50 mg	In stock	$ 296.00
100 mg	In stock	$ 383.00
1 mL * 10 mM (in DMSO)	In stock	$ 47.00

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Purity: 99.61%

Purity: 98.31%

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Description	WYE-354(IC50=5 nM) is an effective, selective and ATP-competitive mTOR inhibitor. It blocks mTORC2/P-AKT(S473) and mTORC1/P-S6K(T389), not P-AKT(T308). The selectivity for mTOR is higher than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
Targets&IC50	mTOR:5 nM, PI3Kγ:7.37 μM, PI3Kα:1.89 μM
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.
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.
Kinase Assay	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.
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.

Molecular Weight	495.53
Formula	C24H29N7O5
CAS No.	1062169-56-5

Storage

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

Solubility Information

DMSO: 92 mg/mL (185.7 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Yu K, et al. Cancer Res, 2009, 69(15), 6232-6240. 2. Dormond-Meuwly A, et al. Biochem Biophys Res Commun, 2011, 407(4), 714-719.

Citations

1. Chen W, Liao Y, Sun P, et al.Construction of an ER stress-related prognostic signature for predicting prognosis and screening the effective anti-tumor drug in osteosarcoma.Journal of Translational Medicine.2024, 22(1): 1-19.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Kinase Inhibitor Library Stem Cell Differentiation Compound Library Oxidation-Reduction Compound Library Anti-Ovarian Cancer Compound Library Neuronal Differentiation Compound Library Anti-Pancreatic Cancer Compound Library Apoptosis Compound Library Anti-Cancer Metabolism Compound Library

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Keywords

WYE-354 1062169-56-5 Apoptosis Autophagy PI3K/Akt/mTOR signaling PI3K mTOR inhibit WYE354 WYE 354 Inhibitor Mammalian target of Rapamycin inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.