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WYE-354

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Purity:99.61%

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COA HPLC HNMR

WYE-354

Catalog No. T6731Cas No. 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).

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Pack Size	Price	Availability
5 mg	$43	In Stock
10 mg	$77	In Stock
25 mg	$158	In Stock
50 mg	$296	In Stock
100 mg	$383	In Stock
1 mL x 10 mM (in DMSO)	$47	In Stock

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Product Introduction

Bioactivity

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	PI3Kα:1.89 μM, mTOR:5 nM, PI3Kγ:7.37 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.

Chemical Properties

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

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0180 mL	10.0902 mL	20.1804 mL	100.9021 mL
5 mM	0.4036 mL	2.0180 mL	4.0361 mL	20.1804 mL
10 mM	0.2018 mL	1.0090 mL	2.0180 mL	10.0902 mL
20 mM	0.1009 mL	0.5045 mL	1.0090 mL	5.0451 mL
50 mM	0.0404 mL	0.2018 mL	0.4036 mL	2.0180 mL
100 mM	0.0202 mL	0.1009 mL	0.2018 mL	1.0090 mL

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In Vivo Formulation Calculator (Clear solution)

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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Tech Support

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