Product Description
KU0063794 is an azaquinazoline-based [1], potent and highly selective inhibitor of mTORC1/2 with IC50 values of ~10 nM. [2] in a kinase panel at 1 uM KU0063794, none of the kinases, including the PI3K family, were inhibited, with the exception of MAPK kinase-1 which was decreased ~55%. [1] In HEK-293 cells in the presence of serum, KU0063794 inhibited S6K1 phosphorylation at Thr389 at concentrations as low as 30 nM. Consequently, inhibition was also observed at Thr229, along with ribosomal S6 protein. KU0063794 was also shown to inhibit phosphorylation of Akt at Thr308 at an IC50 of 86 nM. [3] In cell cycle studies, cell growth was inhibited and cells in the G1 phase were increased two-fold. [2]
Technical information:
| Chemical Formula: | C25H31N5O4 | |
| CAS #: | 938440-64-3 | |
| Molecular Weight: | 465.54 | |
| Purity: | > 99% | |
| Appearance: | Yellow | |
| Chemical Name: | (5-(2-((2S,6R)-2,6-dimethylmorpholino)-4-morpholinopyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol | |
| Solubility: | Up to 30 mM in DMSO | |
| Synonyms: | KU-0063794, KU-63794, KU0063794, KU63794 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature. Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Malagu et al., The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase. Bioorg. Med. Chem. Lett. 2009, 19, 5950-5953. Pubmed ID: 19762236 |
| 2. | Garcia-Martinez et al., Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem. J. 2009, 421, 29-42. Pubmed ID: 19402821 |
| 3. | Liu et al., Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. J. Biol. Chem. 2012, 287(13), 9742-9752. Pubmed ID: 22223645 |
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