Cat. No.: HY-10044

WYE-132

(Synonyms: WYE-125132)

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC₅₀: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibits mTORC1 and mTORC2.

For research use only. We do not sell to patients.

Purity: 99.90%
CAS No.: 1144068-46-1
Formula: C₂₇H₃₃N₇O₄
Molecular Weight:519.60

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

WYE-132 Chemical Structure

CAS No.: 1144068-46-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

mTOR

0.19 nM (IC₅₀)

mTORC1

mTORC2

PI3Kα

1.179 μM (IC₅₀)

PI3Kδ

2.38 μM (IC₅₀)

hSMG1

1.25 μM (IC₅₀)

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	0.12 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human 786-0 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human 786-0 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
A498	IC₅₀	>20 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 1 days by MTS assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 1 days by MTS assay	[PMID: 20068177]
A498	IC₅₀	0.1 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 3 days by MTS assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 3 days by MTS assay	[PMID: 20068177]
A498	IC₅₀	0.11 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
A498	IC₅₀	2.5 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 2 days by MTS assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 2 days by MTS assay	[PMID: 20068177]
A549	IC₅₀	0.102 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
BT-549	IC₅₀	0.037 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
HCT-116	IC₅₀	0.38 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
HeLa	IC₅₀	0.055 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
LNCaP	IC₅₀	0.002 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
LNCaP	IC₅₀	2 nM Compound: 8a	Cytotoxicity against human LNCAP cells Cytotoxicity against human LNCAP cells	[PMID: 20089401]
MDA-MB-231	IC₅₀	0.06 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
MDA-MB-361	IC₅₀	0.012 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human MDA-MB-361 cells assessed as cell growth inhibition incubated for 3 days by MTS assay Antiproliferative activity against human MDA-MB-361 cells assessed as cell growth inhibition incubated for 3 days by MTS assay	[PMID: 20068177]
MDA-MB-361	IC₅₀	0.024 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human MDA-MB-361 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human MDA-MB-361 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
MDA-MB-361	IC₅₀	0.05 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human MDA-MB-361 cells assessed as cell growth inhibition incubated for 2 days by MTS assay Antiproliferative activity against human MDA-MB-361 cells assessed as cell growth inhibition incubated for 2 days by MTS assay	[PMID: 20068177]
MDA-MB-361	IC₅₀	20 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human MDA-MB-361 cells assessed as cell growth inhibition incubated for 1 days by MTS assay Antiproliferative activity against human MDA-MB-361 cells assessed as cell growth inhibition incubated for 1 days by MTS assay	[PMID: 20068177]
MDA-MB-468	IC₅₀	0.025 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
MG-63	IC₅₀	0.025 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human MG-63 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human MG-63 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
NCI-H157	IC₅₀	0.145 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human NCI-H157 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human NCI-H157 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
NCI-H1975	IC₅₀	0.07 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
NCI-H460	IC₅₀	0.3 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]
U-87MG ATCC	IC₅₀	0.065 μM Compound: Chemical Probe: WYE-125132	Antiproliferative activity against human U-87MG cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay Antiproliferative activity against human U-87MG cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay	[PMID: 20068177]

In Vitro

WYE-132 (WYE-125132) potently inhibits recombinant mTOR via an ATP-competitive mechanism. WYE-132 is a potent antiproliferative agent against a panel of cancer cell lines with IC₅₀ values generally in the nanomolar range. In the typical 3-day dose-response studies, WYE-132 exhibits a more profound antiproliferative activity than CCI-779 in MDA361 and other cells, as shown by the sharper inhibition at doses up to 10 μM. Fluorescence-activated cell sorting (FACS) analysis of inhibitor-treated (1 μM, 24 hours) MDA468, PC3MM2, U87MG, A549, and HCT116 cells indicates that WYE-132 elicits a more profound increase in G₁-phase and a reduction in S-phase cells than CCI-779. The WYE-132-induced cell death is evident at 10 and 30 nM (6.2% and 13%, respectively) and is dose dependent, reaching 47% at 1 μM and 59% at 3 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

A single i.v. administration of 50 mg/kg WYE-132 (WYE-125132) into tumor-bearing mice leads to suppression of P-S6K(T389) and P-AKT(S473) for at least 8 hours in PC3MM2, MDA361, HCT116, and HT29 tumors, whereas the steady-state level of P-AKT(T308) is not significantly reduced, indicating that the antitumor efficacy of WYE-132 under such dosing regimens reflects the suppression of mTOR rather than PI3K. Oral administration of WYE-132 causes dose-dependent tumor growth delay in the PI3K/mTOR- and HER2-hyperactive MDA361 tumors with significant antitumor activity at 5 mg/kg, which correlates with a suppression P-S6 and P-AKT(S473) but not P-AKT(T308). An optimal dose of 50 mg/kg WYE-132 induces a substantial regression of large MDA361 tumors. WYE-132 also causes a potent and substantial tumor growth delay in the PTEN-null U87MG glioma^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1144068-46-1
Appearance Solid
Molecular Weight 519.60
Formula C₂₇H₃₃N₇O₄
Color White to gray
SMILES

O=C(NC1=CC=C(C2=NC(N3CC4CCC(C3)O4)=C5C(N(N=C5)C6CCC7(CC6)OCCO7)=N2)C=C1)NC
Synonyms

WYE-125132
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Cell Syst

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]

2020 Jan 22;10(1):66-81.e11. PMID: 31812693
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
Patent

US20160089377A1.

WYE-132 purchased from MedChemExpress. Usage Cited in: Patent. US20160089377A1.

Treatment with WYE125132 rescues cellular, synaptic and molecular abnormalities in Cntnap2 mutants. Bar graphs (top) indicate that the dramatic increase in phosphorylation of S6 (Phospho-S6: S6) in the cortex of Cntnap2^−/− and Cntnap2^+/− mice is completely reversed with by treatment with WYE125132. In Bar graphs, each pair reflects untreated (left) and treated (right) values. Representative immunoblots are shown (bottom).

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (48.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9246 mL

9.6228 mL

19.2456 mL

5 mM

0.3849 mL

1.9246 mL

3.8491 mL

10 mM

0.1925 mL

0.9623 mL

1.9246 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration Concentration

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Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocol

Cell Assay^[1]

Cell lines of MDA-MB-361, MDA-MB-231, MDA-MB-468, BT549, LNCap, A549, H1975, H157, H460, U87MG, A498, 786-O, HCT116, MG63, Rat1, HEK293, HeLa and PC3MM2 are used. MDA361 cells are treated for 3 d with CCI-779 and WYE-132 (0.1 nM, 1 nM, 10 nM,100 nM, 1000 nM 10μM and 100μM). Cell growth assays and IC₅₀ determination are performed. For immunoblotting, cultured cells are treated as indicated. Total cell lysates are prepared using NuPAGE lithium dodecyl sulfate sample buffer and immunoblotted with various antibodies^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
For mTOR biomarker studies, various tumors (400 mm³) grown s.c. in female nude mice are dosed by a single i.v. or oral injection with vehicle or WYE-125132 formulated in 5% ethanol, 2% Tween 80, and 5% polyethylene glycol-400. Tumor lysates are prepared and immunoblotted. For efficacy studies, nude mice bearing U87MG, MDA361, H1975, A549, A498, or 786-O tumors are staged and randomized into treatment groups (n=10). Mice are dosed orally with vehicle or WYE-125132 following qd x5 cycle regimen (5 d on, 2 d off) for up to four cycles. Temsirolimus/CCI-779 is formulated as WYE-132 and dosed i.v. once weekly. Bevacizumab is formulated in PBS and dosed i.p. via its clinical regimen (200 μg/mouse; once weekly). Tumor growth is monitored and analyzed.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Yu K, et al. Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2.Cancer Res. 2010 Jan 15;70(2):621-631. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.9246 mL	9.6228 mL	19.2456 mL	48.1139 mL
	5 mM	0.3849 mL	1.9246 mL	3.8491 mL	9.6228 mL
	10 mM	0.1925 mL	0.9623 mL	1.9246 mL	4.8114 mL
	15 mM	0.1283 mL	0.6415 mL	1.2830 mL	3.2076 mL
	20 mM	0.0962 mL	0.4811 mL	0.9623 mL	2.4057 mL
	25 mM	0.0770 mL	0.3849 mL	0.7698 mL	1.9246 mL
	30 mM	0.0642 mL	0.3208 mL	0.6415 mL	1.6038 mL
	40 mM	0.0481 mL	0.2406 mL	0.4811 mL	1.2028 mL

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WYE-132

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Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

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Cancer Stem Cells Compound Library

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Highly Selective Inhibitors Library

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Cell Death Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

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Publications Citing Use of MedChemExpress (MCE) WYE-132

All mTOR Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

WYE-132 Related Classifications

Cat. No.: HY-10044