WYE-354

Catalog No.S1266

WYE-354 Chemical Structure

Molecular Weight(MW): 495.53

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).

Size Price Stock Quantity  
In DMSO USD 240 In stock
USD 120 In stock
USD 210 In stock
USD 770 In stock
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4 Customer Reviews

  • WYE-354 is cytotoxic and anti-proliferative when adding to cultured human colon cancer cells. Established human colon cancer cell lines (HCT-116, HT-29, Caco-2, LoVo, and DLD-1), three lines of primary human colon cancer cells (P1, P2, and P3), or non-cancerous NCM460 colon epithelial cells were treated with applied concentration of WYE-354 ("WYE") for indicated time period, cell survival was tested by MTT assay (a, b, d, f), and cell proliferation was evaluated by clonogenicity assay (c, e). The data in this and all following figures were representatives of three different experiments. n = 5 for each assay. The values were expressed as the means ± SD (same for all figures). "C" stands for untreated control group (same for all figures). *p<0.05 vs. "C" group

    Tumour Biol, 2016, 37(9):11743-11752. WYE-354 purchased from Selleck.

    After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WYE-354 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

    Dr. Zhang of Tianjin Medical University. WYE-354 purchased from Selleck.

  • For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WYE-354 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.

    Dr. Yong-Weon Yi from Georgetown University Medical Center. WYE-354 purchased from Selleck.

    HCT116 were left untreated (C) or stimulated for 5 h with serum (FBS) and rapamycin or WYE-354 at the indicated concentrations.

    Dr. Pierre P. Roger from Free University of Brussels. WYE-354 purchased from Selleck.

Purity & Quality Control

Choose Selective mTOR Inhibitors

Biological Activity

Description 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).
Targets
mTOR [1]
()
5 nM
In vitro

WYE-354 also inhibits several PI3Ks at micromolar levels. In HEK293 cells, WYE-354 (0.2 μM–5 μM) effectively inhibits both mTORC1 and mTORC2. WYE-354 (0.3 μM–10 μM) significantly blocks mTOR signaling and Akt activation in U87MG and MDA361 cells. Furthermore, WYE-354 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 WYE-354 is accompanied by G1 cell cycle arrest and caspases activation. [1] In endothelial HUVEC cells, WYE-354 (10 nM–1 μM) also inhibits both mTORC1 and mTORC2 signaling, as revealed by dephosphorylation of S6 ribosomal protein and Akt, respectively. Furthermore, WYE-354 (10 nM–1 μM) activates mitogen-activated protein kinase (MAPK) signaling, which may be due to its inhibition of mTORC1. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells NH70d|ZHfW6ldHnvckBie3OjeR?= NHj5eJJKdmirYnn0bY9vKG:oIH\sZYcufGGpZ3XkJJRzfW6lYYTl[EBpfW2jbjDtWG9TKChzM{[wMVI2PDlrIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYomgSGVNTkmDIHHzd4F6NCCLQ{WwQVAvODB2MzFOwG0> NH\oOWQyQTZ2NUS0PC=>
LNCAP cells NU\mRmRMS3m2b4TvfIlkcXS7IHHzd4F6 MnjZN{Bl[Xm| NHftfVhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNVkODUDDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvOzV3IN88US=> M3r1OVE6PjR3NES4

... Click to View More Cell Line Experimental Data

In vivo In a mice xenograft model of PTEN-null PC3MM2 tumor, WYE-354 (50 mg/kg) effectively inhibits mTOR signaling and tumor growth. [1]

Protocol

Kinase Assay:[1]
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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 WYE-354. 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.
Cell Research:[1]
+ Expand
  • Cell lines: Tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, DU145, A498, and HCT116
  • Concentrations: 0–50 μM, dissolved in DMSO
  • Incubation Time: 72 hours
  • Method: Cells 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. Viable cell densities are determined 72 hours later by MTS assay employing a CellTiter 96 kit. The effect of each treatment is calculated as percent of control growth relative to the DMSO-treated cells grown in the same culture plate. Inhibitor dose response curves are plotted for determination of IC50 values.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Nude mice (BALB/c, nu/nu, female) bearing PC3MM2 xenograft
  • Formulation: Dissolved in 5% ethanol, 5% polysorbate 80, 5% PEG-400
  • Dosages: 50 mg/kg
  • Administration: Administered via intraperitoneal injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 99 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 495.53
Formula

C24H29N7O5

CAS No. 1062169-56-5
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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mTOR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID