Home Tools

KU-0063794

Catalog No. T2475 CAS 938440-64-3

KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2.

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

KU-0063794, CAS 938440-64-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 52.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 132.00
50 mg	In stock	$ 233.00
100 mg	In stock	$ 432.00
500 mg	In stock	$ 982.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

Bulk Inquiry

Select Batch

Purity: 100%

Purity: 98.35%

Purity: 97.29%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2.
Targets&IC50	mTORC1:10 nM, mTORC2:10 nM
In vivo	KU-0063794, unlike Rapamycin, inhibits SGK1 activity and Ser422 phosphorylation in a dose-dependent manner, as well as the phosphorylation of its physiological substrate NDGR1, to the same extent as it does S6K1 and Akt. However, KU-0063794 does not inhibit the phosphorylation and activation of ERK or RSK induced by phorbol ester. Compared to Rapamycin, KU-0063794 demonstrates significantly greater potency in inducing complete dephosphorylation of 4E-BP1 at Thr37, Thr46, and Ser65. It also inhibits the growth of both wild-type and mLST8-deficient MEFs cells, and induces a more pronounced G1 phase cell cycle arrest than Rapamycin. KU-0063794 shows higher specificity towards mTOR compared to the mTOR inhibitor PP242, as it does not affect PI3K or any other of the 76 kinases tested. In HEK-293 cells, 30 nM KU-0063794 is sufficient to rapidly abolish S6K1 activity by blocking phosphorylation at the hydrophobic motif (Thr389) and subsequent phosphorylation at the T-loop residue (Thr229). At concentrations of 100-300 nM, KU-0063794 also completely inhibits amino acid-induced phosphorylation of S6K1 and S6 protein. Similarly, KU-0063794 inhibits the phosphorylation of mTORC1 at Ser2448 and mTORC2 at Ser2481 in a dose- and time-dependent manner.
Kinase Assay	mTOR complexes kinase assays: HEK-293 cells are freshly lysed in Hepes lysis buffer. Lysate (1-4 mg) is pre-cleared by incubating with 5-20 μL of Protein G-Sepharose conjugated to pre-immune IgG. The lysate extracts are then incubated with 5-20 μL of Protein G-Sepharose conjugated to 5-20 μg of either anti-Rictor or anti-Raptor antibody, or pre-immune IgG. All antibodies are covalently conjugated to Protein G-Sepharose. Immunoprecipitations are carried out for 1 hour at 4 °C on a vibrating platform. The immunoprecipitates are washed four times with Hepes lysis buffer, followed by two washes with Hepes kinase buffer. For Raptor immunoprecipitates used for phosphorylating S6K1, for the initial two wash steps the buffer includes 0.5 M NaCl to ensure optimal kinase activity. GST-Akt1 is isolated from serum-deprived HEK-293 cells incubated with PI-103 (1 μM for 1 hour). GST-S6K1 is purified from serum-deprived HEK-293 cells incubated with rapamycin (0.1 μM for 1 hour). mTOR reactions are initiated by adding 0.1 mM ATP and 10 mM MgCl2 in the presence of various concentrations of KU-0063794 and GST-Akt1 (0.5 μg) or GST-S6K1 (0.5 μg). Reaction are carried out for 30 minutes at 30 °C on a vibrating platform and stopped by addition of SDS sample buffer. Reaction mixtures are then filtered through a 0.22-μm-poresize Spin-X filter and samples are subjected to electrophoresis and immunoblot analysis with the indicated antibodies.
Cell Research	Cells are treated with KU-0063794 for 24, 48, and 72 hours, and the medium is changed every 24 hours with freshly dissolved KU-0063794. For the measurement of cell growth, cells are washed once with PBS, and fixed in 4% (v/v) paraformaldehyde in PBS for 15 minutes. After washing once with water, the cells are stained with 0.1% Crystal Violet in 10% ethanol for 20 minutes and washed three times with water. Crystal Violet is extracted from cells with 0.5 mL of 10% (v/v) ethanoic (acetic) acid for 20 minutes. The eluate is then diluted 1:10 in water and absorbance at 590 nm is quantified. For the assessment of cell cycle distribution, cells are harvested by trypsinization, washed once in PBS, and re-suspended in ice-cold aq. 70% (v/v) ethanol. Cells are washed twice in PBS plus 1% (w/v) BSA and stained for 20 minutes in PBS plus 0.1% (v/v) Triton X-100 containing 50 g/mL propidium iodide and 50 g/mL RNase A. The DNA content of cells is determined using a FACSCalibur flow cytometer and CellQuest software. Red fluorescence (585 nm) is acquired on a linear scale, and pulse width analysis is used to exclude doublets. Cell-cycle distribution is determined using FlowJo software.(Only for Reference)

Molecular Weight	465.54
Formula	C25H31N5O4
CAS No.	938440-64-3

Storage

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

Solubility Information

DMSO: 4.7 mg/mL (10 mM)

References and Literature

1. García-Martínez JM, et al. Biochem J, 2009, 421(1), 29

Citations

1. Nian Z, Zheng X, Dou Y, et al. Rapamycin pretreatment rescues the bone marrow AML cell elimination capacity of CAR-T cells. Clinical Cancer Research. 2021

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Kinase Inhibitor Library Highly Selective Inhibitor Library Inhibitor Library Anti-Cancer Metabolism Compound Library Bioactive Compound Library Reprogramming Compound Library Anti-Pancreatic Cancer Compound Library Anti-Breast Cancer Compound Library Anti-Prostate Cancer Compound Library

Related Products

Related compounds with same targets

DS-7423 mTOR inhibitor-14 Onjisaponin B ETP-46464 Torin 2 mTOR inhibitor-12 LY 303511 hydrochloride DMH-25

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

KU-0063794 938440-64-3 PI3K/Akt/mTOR signaling mTOR Inhibitor KU0063794 Mammalian target of Rapamycin KU 0063794 inhibit inhibitor

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