Home Tools

WYE-132

Catalog No. T6346 CAS 1144068-46-1

Synonyms: WYE 125132, WYE125132, WYE-125132

WYE-125132 (WYE-132 (WYE-125132)) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

WYE-132, CAS 1144068-46-1

Pack Size	Availability	Price/USD	Quantity
2 mg	5 days	$ 53.00

Bulk Inquiry

Biological Description

Chemical Properties

Storage & Solubility Information

Description	WYE-125132 (WYE-132 (WYE-125132)) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.
Targets&IC50	mTOR:0.19 nM
In vitro	WYE-125132 potently and ATP-competitively inhibits recombinant mTOR kinase with IC50 of 0.19 nM and also shows the high selectivity over various PI3Ks and a panel of 230 protein kinases. [1] In vitro, WYE-125132 exhibits a significant anti-proliferative activity against a panel of tumor cell lines with IC50 ranging from 2 nM (LNCap) to 380 nM (HTC116). Besides, WYE-125132 also causes cell cycle progression, induction of apoptosis, and inhibition of protein synthesis and cell size. [1] WYE-125132 results in a significant reduction in the synthesis of pre-tRNALeu by 72%, 80%, and 53% in actively proliferating cells of MG63, MDA361, and HEK293, respectively by inhibiting mTORC1. Moreover, WYE-125132 is also found to induce the dephosphorylation of Maf1 (negative regulator of Pol III transcription) and its accumulation in the nucleus. [2]
In vivo	WYE-125132 (5 mg/kg p.o.) produces significant antitumor activity and causes dose-dependent tumor growth delay in the PI3K/mTOR- and HER2-hyperactive MDA361 tumor model. In addition, WYE-125132 also shows potent antitumor efficacy in the PTEN-null glioma U87 mg, non-small cell lung cancer H1975 and A549 models. [1]
Kinase Assay	Kinase assays: mTOR enzyme assays via dissociation-enhanced lanthanide fluorescent immunoassay (DELFIA), ATP matrix assays, and mTOR immune-complex kinase assays are performed as follows. The endogenous TOR of LNCap cell lysate is immunoprecipitated by anti-FRAP/TOR (N-19). Cell lysate (1.0 mg) is mixed with 4 μg antibody coupled to protein-G/A agarose in 1 mL lysis buffer. The immune-complexes are washed sequentially with lysis buffer, lysis buffer plus 500 mM KCl, and kinase buffer wash. The immune-complexes are subjected to kinase reaction for 30 minutes at 30 °C in a final volume of 50 μL containing 10 mM Hepes (pH 7.4), 50 mM NaCl, 50 mM β-glycerophosphate, and 0.5 μM microcystin LR, 1 mM DTT, 10 mM MnCl2, 100 μM ATP, 1 μg His6-S6K or 1 μg His6-4EBP1. Kinase reactions (immune-complex and purified enzymes) are terminated by NuPAGE LDS sample buffer and resolved in a 4-12% NuPAGE Bis-Tris gel for Western blotting with anti-P(T389)-p70S6K and anti-P(T46)-4EBP1, anti-FRAP/TOR (N-19), anti-FLAG M2, and anti-His6 (Clone His-1). In the radioactive assay, 10 μCi [γ-32P]ATP (3000 Ci/mmol) and 100 μM cold ATP are used. 32P-labeled products are resolved by SDS-PAGE and subjected to autoradiogram to Kodak X-ray films.
Cell Research	Cell lines of MDA-MB-361, MDA-MB-231, MDA-MB-468, BT549, LNCap, A549, H1975, H157, H460, U87 mg, A498, 786-O, HCT116, MG63, Rat1, HEK293, and HeLa are obtained from the American Type Culture Collection. Cell growth assays and IC50 determination are described as follows. For tumor cell growth assays, cells are plated in 96-well culture plates at 1000 to 3000 cells per well for 24 hours, treated with DMSO or various doses of WYE-125132. Viable cell densities are determined three days later by MTS assay employing an assay kit following the kit assay protocol. 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)

Synonyms	WYE 125132, WYE125132, WYE-125132
Molecular Weight	519.6
Formula	C27H33N7O4
CAS No.	1144068-46-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 96 mg/mL (184.8 mM)

Ethanol: <1 mg/mL

H2O: <1 mg/mL

References and Literature

1. Yu K, et al. Cancer Res. 2010, 70(2), 621-631. 2. Shor B, et al. J Biol Chem. 2010, 285(20), 15380-15392. 3. Wang Z, Feng J, Yu J, et al. FKBP12 mediates necroptosis by initiating RIPK1–RIPK3–MLKL signal transduction in response to TNF receptor 1 ligation[J]. Journal of cell science. 2019 May 20;132(10). pii: jcs227777.

Citations

1. Wang Z, Feng J, Yu J, et al. FKBP12 mediates necroptosis by initiating RIPK1-RIPK3-MLKL signal transduction in response to TNF receptor 1 ligation. Journal of Cell Science. 2019, 132(10): jcs227777

Related Products

Related compounds with same targets

TJ191 AZD-8055 Bryonolic acid 5-LOX-IN-2 Isobavachalcone Telomerase-IN-4 Ripretinib Rhosin hydrochloride

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

WYE-132 1144068-46-1 Apoptosis PI3K/Akt/mTOR signaling mTOR Inhibitor inhibit Mammalian target of Rapamycin WYE 125132 WYE 132 WYE125132 WYE-125132 WYE132 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.