WYE-354
Based on 7 publication(s) in Google Scholar
WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.03%
- No. CAS: 1062169-56-5
- Fòrmula: C24H29N7O5
- Peso molecular:495.53
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) WYE-354
More- Acta Pharm Sin B. 2025 Jan;15(1):133-150. [Abstract]
- Int J Mol Sci. 2020 Feb 19;21(4):1387. [Abstract]
- Front Pharmacol. 2020 Nov 11:11:580407. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2018 May;1865(5):709-720. [Abstract]
- ACS Chem Biol. 2012 Jun 15;7(6):982-7. [Abstract]
- bioRxiv. 2024 September 07.
Actividad biológica
|
mTOR 5 nM (IC50) |
mTORC1 |
mTORC2 |
PI3K alpha 1.89 μM (IC50) |
PI3K gamma 7.37 μM (IC50) |
Autophagy |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
4.3 nM
Compound: 19
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Inhibition of flag-tagged truncated human mTOR (1360-2549) expressed in HEK293 cells by DELFIA assay
Inhibition of flag-tagged truncated human mTOR (1360-2549) expressed in HEK293 cells by DELFIA assay
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[PMID: 19645448] |
| LNCaP | IC50 |
355 nM
Compound: 19
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Cytotoxicity against human LNCAP cells after 3 days by MTS assay
Cytotoxicity against human LNCAP cells after 3 days by MTS assay
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[PMID: 19645448] |
In the DELFIA measuring His6-S6K1 T389 phosphorylation, WYE-354 inhibits recombinant mTOR enzyme with an IC50 of 5 nM[1]. Cell viability is analyzed by MTS assay. G-415 and TGBC-2TKB cell lines are treated with increasing concentrations of WYE-354 (0.1, 1, 5 and 10 μM) for 24, 48, and 72 hours. WYE-354 significantly reduces cell viability starting at a 1 μM concentration after a 24 hours exposure, in both studied cell lines (P<0.001). A decrease in cell viability is not observed at a dose of 100 nM, except for the TGBC-2TKB cell line after 72 hours of treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1062169-56-5
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Appearance Solid
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Peso molecular 495.53
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Fòrmula C24H29N7O5
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Color White to off-white
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SMILES
COC(NC1=CC=C(C=C1)C2=NC3=C(C(N4CCOCC4)=N2)C=NN3C5CCN(CC5)C(OC)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Acta Pharm Sin B
GSFM: A genome-scale functional module transformation to represent drug efficacy for in silico drug discovery. [Abstract]2025 Jan;15(1):133-150. PMID: 40041913 -
Int J Mol Sci
Overexpression of ABCB1 Transporter Confers Resistance to mTOR Inhibitor WYE-354 in Cancer Cells. [Abstract]2020 Feb 19;21(4):1387. PMID: 32092870 -
Front Pharmacol
CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]2020 Nov 11:11:580407. PMID: 33343350 -
Molecules
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]2020 Apr 23;25(8):1980. PMID: 32340370 -
Biochim Biophys Acta Mol Cell Res
Low shear stress induces vascular eNOS uncoupling via autophagy-mediated eNOS phosphorylation. [Abstract]2018 May;1865(5):709-720. PMID: 29466710 -
ACS Chem Biol
Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae. [Abstract]2012 Jun 15;7(6):982-7. PMID: 22496512 -
Solvente y solubilidad
DMSO : 6.67 mg/mL (13.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.67 mg/mL (1.35 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.67 mg/mL (1.35 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
The routine inhibitor assays are performed in 96-well plates for 2 h at room temperature in 25 μL containing 6 nM Flag-TOR(3.5) (estimated 5-10% purity), 1 μM His6-S6K and 100 μM ATP. The assays are performed and detected by DELFIA employing the Euphospho-p70S6K T389 antibody. Some assays employ a commercially purchased batch of mTOR. 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 contain 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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
G-415 and TGBC-2TKB cell lines are plated onto 96 well plates at a density of 2×103 cells per well. After an overnight attachment period cells are treated with WYE-354. The number of viable cells is determined at certain intervals using CellTiter 96 Aqueous One Solution Cell Proliferation assay. 20 μL CellTiter 96 solution is added to each well and the plates are incubated for 2 hour after which the absorbance of each well is read at a wavelength of 490 nm using a multiwell plate reader. All assays are performed in quintuplicate, and each assay is repeated three times[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
8 to 12-week- old NOD-SCID mice are subcutaneously injected in one flank with either 2×106 or 5×106 cells of G-415 or TGBC2TKB, respectively, and re-suspended in 200 μL of PBS with 30% of Matrigel. When the average tumor reach 100 mm3, mice are randomly separated into four groups and treated with Rapamycin or WYE-354 and its respective vehicles. Rapamycin is administered at a daily intraperitoneal (i.p) dose of 10 mg/kg for 5 days per week for 3 weeks, while WYE-354 is administrated at a daily i.p dose of 50 mg/kg for 5 days. Tumor volumes are estimated twice a week.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Yu K et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009 Aug 1;69(15):6232-40. [Content Brief]
[2]. Weber H, et al. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice. Oncotarget. 2015 Oct 13;6(31):31877-88. [Content Brief]
[3]. Lijun Wang, et al. Autophagy inhibition sensitizes WYE-354-induced anti-colon cancer activity in vitro and in vivo. Tumour Biol. 2016 Sep;37(9):11743-11752. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0180 mL | 10.0902 mL | 20.1804 mL | 50.4510 mL |
| 5 mM | 0.4036 mL | 2.0180 mL | 4.0361 mL | 10.0902 mL | |
| 10 mM | 0.2018 mL | 1.0090 mL | 2.0180 mL | 5.0451 mL |
WYE-354 Related Classifications
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