KU-0063794

Name: KU-0063794
Brand: MedChemExpress
SKU: HY-50710
Rating: 5.0 (13 reviews)

Cat. No.: HY-50710 Purity: 99.55%: FAQs
Data Sheet SDS COA Handling Instructions

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KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC₅₀s of 10 nM.

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

KU-0063794 Chemical Structure

CAS No. : 938440-64-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 67	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 67	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 528	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 13 publication(s) in Google Scholar

13 Publications Citing Use of MCE KU-0063794

•Patent. US20180263995A1.

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mTOR mTORC1 mTORC2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC₅₀s of 10 nM.

IC₅₀ & Target^[1]

mTORC1

10 nM (IC₅₀)

mTORC2

10 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.003 μM Compound: 31	Inhibition of recombinant FLAG-tagged mTOR expressed in HEK293 cells using biotinylated p70S6K substrate after 2 hrs by alphascreen competition assay Inhibition of recombinant FLAG-tagged mTOR expressed in HEK293 cells using biotinylated p70S6K substrate after 2 hrs by alphascreen competition assay	[PMID: 19762236]
HEK293	IC₅₀	10 nM Compound: 16; Ku-0063794	Inhibition of mTORC1 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay Inhibition of mTORC1 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay	[PMID: 29211480]
HEK293	IC₅₀	10 nM Compound: 16; Ku-0063794	Inhibition of mTORC2 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay Inhibition of mTORC2 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay	[PMID: 29211480]
HeLa	IC₅₀	0.016 μM Compound: 31	Inhibition of mTOR in human HeLa cells using 4E-BP1 substrate by ELISA Inhibition of mTOR in human HeLa cells using 4E-BP1 substrate by ELISA	[PMID: 19762236]
MDA-MB-468	IC₅₀	0.24 μM Compound: Ku-0063794	Inhibition of mTORC2 in human MDA-MB-468 cells assessed as reduction of AKT phosphorylation at Ser473 after 2 hrs Inhibition of mTORC2 in human MDA-MB-468 cells assessed as reduction of AKT phosphorylation at Ser473 after 2 hrs	[PMID: 23375793]
MDA-MB-468	IC₅₀	0.66 μM Compound: Ku-0063794	Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction of pS6 phosphorylation at Ser235/236 after 2 hrs Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction of pS6 phosphorylation at Ser235/236 after 2 hrs	[PMID: 23375793]
T47D	GI₅₀	0.35 μM Compound: 31	Antiproliferative activity against human T47D cells after 120 hrs by SRB assay Antiproliferative activity against human T47D cells after 120 hrs by SRB assay	[PMID: 19762236]
U-87MG ATCC	IC₅₀	0.1 μM Compound: 31	Inhibition of mTORC1 in human U87MG cells assessed as phosphorylated S6 ribosomal protein (Ser235/236) level after 2 hrs by Western blotting Inhibition of mTORC1 in human U87MG cells assessed as phosphorylated S6 ribosomal protein (Ser235/236) level after 2 hrs by Western blotting	[PMID: 19762236]
U-87MG ATCC	IC₅₀	0.15 μM Compound: 31	Inhibition of mTORC2 in human U87MG cells assessed as phosphorylated AKT (Ser473) level after 2 hrs by Western blotting Inhibition of mTORC2 in human U87MG cells assessed as phosphorylated AKT (Ser473) level after 2 hrs by Western blotting	[PMID: 19762236]

In Vitro

Ku-0063794 is cell permeant, suppresses activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not RSK (ribosomal S6 kinase), an AGC kinase not regulated by mTOR. Ku-0063794 also inhibits phosphorylation of the T-loop Thr308 residue of Akt phosphorylated by PDK1 (3-phosphoinositide-dependent protein kinase-1). Ku-0063794 induces a much greater dephosphorylation of the mTORC1 substrate 4E-BP1 (eukaryotic initiation factor 4E-binding protein 1) than rapamycin, even in mTORC2-deficient cells, suggesting a form of mTOR distinct from mTORC1, or mTORC2 phosphorylates 4E-BP1. Ku-0063794 also suppresses cell growth and induced a G1-cell-cycle arrest^[1]. Ku0063794 does not alter nuclear phospho-Mst1-Thr-120 levels in LNCaP cell nuclei, whereas Ku0063794 or CCI-779 increases phospho-Mst1-Thr-120 levels in C4-2 cell nuclei^[2]. The combination of GDC-0941 and KU0063794 inhibits the phosphorylation of 4EBP1 and S6 to a similar extent to that caused by single agent NVP-BEZ235 in HCT116, DLD1 and HT29 cell lines^[3].

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

Molecular Weight

465.54

Formula

C₂₅H₃₁N₅O₄

CAS No.

938440-64-3

Appearance

Solid

Color

Light yellow to yellow

SMILES

OCC1=CC(C2=CC=C3C(N=C(N=C3N4CCOCC4)N5C[C@@H](O[C@@H](C5)C)C)=N2)=CC=C1OC

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

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL (35.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1480 mL	10.7402 mL	21.4804 mL
5 mM	0.4296 mL	2.1480 mL	4.2961 mL
10 mM	0.2148 mL	1.0740 mL	2.1480 mL

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (3.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (3.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (3.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 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 (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.55%

Select Batch:

Data Sheet (280 KB) SDS (419 KB)

COA (249 KB) LCMS (270 KB)

Handling Instructions (2659 KB)

References

[1]. Garcia-Martinez et al. Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem.J. (2009)421 29. [Content Brief]

[2]. Collak FK, et al. Threonine-120 phosphorylation regulated by phosphoinositide-3-kinase/Akt and mammalian target of rapamycin pathway signaling limits the antitumor activity of mammalian sterile 20-like kinase 1.J Biol Chem. 2012 Jul 6;287(28):23698-709. E [Content Brief]

[3]. Haagensen EJ, et al. The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition. Br J Cancer. 2012 Apr 10;106(8):1386-94. [Content Brief]

Kinase Assay ^[1]	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 0.5mol/LNaCl 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Garcia-Martinez et al. Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem.J. (2009)421 29. [Content Brief] [2]. Collak FK, et al. Threonine-120 phosphorylation regulated by phosphoinositide-3-kinase/Akt and mammalian target of rapamycin pathway signaling limits the antitumor activity of mammalian sterile 20-like kinase 1.J Biol Chem. 2012 Jul 6;287(28):23698-709. E [Content Brief] [3]. Haagensen EJ, et al. The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition. Br J Cancer. 2012 Apr 10;106(8):1386-94. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1480 mL	10.7402 mL	21.4804 mL	53.7011 mL
	5 mM	0.4296 mL	2.1480 mL	4.2961 mL	10.7402 mL
	10 mM	0.2148 mL	1.0740 mL	2.1480 mL	5.3701 mL
	15 mM	0.1432 mL	0.7160 mL	1.4320 mL	3.5801 mL
	20 mM	0.1074 mL	0.5370 mL	1.0740 mL	2.6851 mL
	25 mM	0.0859 mL	0.4296 mL	0.8592 mL	2.1480 mL
	30 mM	0.0716 mL	0.3580 mL	0.7160 mL	1.7900 mL

KU-0063794 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KU-0063794938440-64-3KU0063794KU 0063794mTORMammalian target of RapamycinInhibitorinhibitorinhibit

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KU-0063794

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KU-0063794 Related Antibodies

13 Publications Citing Use of MCE KU-0063794

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Biological Activity

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Purity & Documentation

References

Customer Review

KU-0063794 Related Antibodies

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Complete Stock Solution Preparation Table

KU-0063794 Related Classifications

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