KU-0063794 is a potent and selective mTOT inhibitor, which inhibits both mTORC1 and mTORC2 with an IC50 of approximately 10 nM, but does not suppress the activity of 76 other protein kinases or seven lipid kinases, including Class 1 PI3Ks (phosphoinositide 3-kinases) at 1000-fold higher concentrations. 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 inhibited phosphorylation of the T-loop Thr308 residue of Akt phosphorylated by PDK1 (3-phosphoinositide-dependent protein kinase-1). Ku-0063794 will be useful in delineating the physiological roles of mTOR and may have utility in treatment of cancers in which this pathway is inappropriately activated.(Source: Biochem J. 2009 Jun 12;421(1):29-42)
MedKoo Cat#: 205776
Name: KU-0063794
CAS#: 938440-64-3
Chemical Formula: C25H31N5O4
Exact Mass: 465.2376
Molecular Weight: 465.54
Elemental Analysis: C, 64.50; H, 6.71; N, 15.04; O, 13.75
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 5.0 | 10.74 | |
| DMF:PBS (pH 7.2) (1:1) | 0.5 | 1.07 | |
| DMSO | 9.8 | 21.12 |
The following data is based on the product molecular weight 465.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
