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KU-0063794

Cat. No. M1731
KU-0063794 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 60  USD60 In stock
5mg USD 55  USD55 In stock
10mg USD 99  USD99 In stock
50mg USD 289  USD289 In stock
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Quality Control & Documentation
Biological Activity

KU-0063794 is a potent and selective mTOR inhibitor with IC50 values of approximately 10 nM for mTORC1 and mTORC2.But KU-0063794 does not inhibit the activity of 76 other protein kinases and seven lipid kinases at 1000-fold higher concentrations. KU-0063794 also inhibited growth of T47D breast cancer cells with a GI50 of 0.35 µM.

Customer Product Validations & Biological Datas
Source J Invest Dermatol (2013). Figure 1. KU-0063794
Method In-Cell Western Blotting
Cell Lines Primary KFs cells
Concentrations 10 μmol/l
Incubation Time 24 h
Results Both AZ compounds showed a significant (P<0.01) reduction of p-mTOR, Rictor, and Raptor immunoreactivity
Protocol (for reference only)
Cell Experiment
Cell lines MEFs cell line
Preparation method Cell growth. MEFs were seeded in 24-well plates (20000 cells per 1.91 cm2 well) and grown overnight in the presence of 10% foetal bovine serum. Cells were then treated in the presence or absence or rapamycin or Ku-0063794 and the medium was changed every 24 h with freshly dissolved inhibitors. Every 24 h of treatment, cells were washed once with PBS, and fixed in 4% (v/v) paraformaldehyde in PBS for 15 min. After washing once with water, the cells were stained with 0.1% Crystal Violet in 10% ethanol for 20 min and washed three times with water. Crystal Violet was extracted from cells with 0.5 ml of 10% (v/v) ethanoic (acetic) acid for 20 min. The eluate was then diluted 1:10 in water, and absorbance at 590 nm was quantified.
Concentrations 3 μM
Incubation time 1, 2 or 3 days
Animal Experiment
Animal models Xenograft Model of RCC
Formulation solubilized in one part DMSO and then diluted (200 µg/100 µl) with 4 parts PEG1500 (50% (w/v) in 75 mM Hepes, pH 8.0, Roche Applied Science)
Dosages 8 mg/kg once daily (five days a week)
Administration intraperitoneal (IP) injection
Chemical Information
Molecular Weight 465.54
Formula C25H31N5O4
CAS Number 938440-64-3
Solubility (25°C) DMSO 15 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Zhang H, et al. PLoS One. A comparison of Ku0063794, a dual mTORC1 and mTORC2 inhibitor, and temsirolimus in preclinical renal cell carcinoma models.

[2] Wahdan-Alaswad RS et al. Mol Cancer Res. Inhibition of mTORC1 kinase activates Smads 1 and 5 but not Smad8 in human prostate cancer cells, mediating cytostatic response to rapamycin.

[3] García-Martínez JM et al. Biochem J. Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR).

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Keywords: KU-0063794 supplier, mTOR, inhibitors, activators


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