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KU-0063794

Cat. No. M1731
KU-0063794 Structure
Size Price Availability Quantity
10mg USD 110 In stock
50mg USD 330 In stock
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Quality Control
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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 465.54
Formula C25H31N5O4
CAS Number 938440-64-3
Purity >99%
Solubility DMSO
Storage at -20°C
References

A comparison of Ku0063794, a dual mTORC1 and mTORC2 inhibitor, and temsirolimus in preclinical renal cell carcinoma models.
Zhang H, et al. PLoS One. 2013;8(1):e54918. PMID: 23349989.

Inhibition of mTORC1 kinase activates Smads 1 and 5 but not Smad8 in human prostate cancer cells, mediating cytostatic response to rapamycin.
Wahdan-Alaswad RS et al. Mol Cancer Res. 2012 Jun;10(6):821-33. PMID: 22452883.

Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR).
García-Martínez JM et al. Biochem J. 2009 Jun 12;421(1):29-42. PMID: 19402821.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: KU-0063794 supplier, mTOR, inhibitors

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