Home PI3K/Akt/mTOR mTOR inhibitor WYE-354

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WYE-354 mTOR inhibitor

Cat.No.S1266

WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
WYE-354 mTOR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 495.53

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Quality Control

Batch: S126601 DMSO]99 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.25%
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99.25

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells Function assay Inhibition of flag-tagged truncated human mTOR (1360-2549) expressed in HEK293 cells by DELFIA assay, IC50=0.0043 μM
LNCAP cells Cytotoxicity assay 3 days Cytotoxicity against human LNCAP cells after 3 days by MTS assay, IC50=0.355 μM
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Solubility

In vitro
Batch:

DMSO : 99 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 495.53 Formula

C24H29N7O5

 Storage (From the date of receipt)
CAS No. 1062169-56-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC(=O)NC1=CC=C(C=C1)C2=NC3=C(C=NN3C4CCN(CC4)C(=O)OC)C(=N2)N5CCOCC5

Mechanism of Action

Targets/IC50/Ki
mTOR
5 nM
In vitro
WYE-354 also inhibits several PI3Ks at micromolar levels. In HEK293 cells, this compound (0.2 μM–5 μM) effectively inhibits both mTORC1 and mTORC2. It (0.3 μM–10 μM) significantly blocks mTOR signaling and Akt activation in U87MG and MDA361 cells. Furthermore, this chemical potently inhibits proliferation in tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, A498, and HCT116, with IC50 values ranging from 0.28 μM to 2.3 μM. The apoptosis induced by this compound is accompanied by G1 cell cycle arrest and caspases activation. In endothelial HUVEC cells, it (10 nM–1 μM) also inhibits both mTORC1 and mTORC2 signaling, as revealed by dephosphorylation of S6 ribosomal protein and Akt, respectively. Furthermore, this chemical (10 nM–1 μM) activates mitogen-activated protein kinase (MAPK) signaling, which may be due to its inhibition of mTORC1.
Kinase Assay
mTOR inhibitor assays
The assays are performed in 96-well plates for 2 hours at room temperature in 25 μL containing 6 nM Flag-TOR(3.5), 1 μM His6-S6K, and 100 μM ATP. The assays are performed and detected by DELFIA employing the Eu-phospho-p70S6K T389 antibody. 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 this compound. The assays contained 12 nM Flag-TOR(3.5), 1 μM His-S6K, and are incubated for 30 min. The assay results are similarly detected by DELFIA and processed for generation of double-reciprocal plots.
In vivo
In a mice xenograft model of PTEN-null PC3MM2 tumor, WYE-354 (50 mg/kg) effectively inhibits mTOR signaling and tumor growth.
References

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