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KU0063794isanazaquinazoline-based[1],potentandhighlyselectiveinhibitorofmTORC1/2withIC50valuesof~10nM.[2]inakinasepanelat1uMKU0063794,noneofthekinases,includingthePI3Kfamily,wereinhibited,withtheexceptionofMAPKkinase-1whichwasdecreased~55%.[1]InHEK-293cellsinthepresenceofserum,KU0063794inhibitedS6K1phosphorylationatThr389atconcentrationsaslowas30nM.Consequently,inhibitionwasalsoobservedatThr229,alongwithribosomalS6protein.KU0063794wasalsoshowntoinhibitphosphorylationofAktatThr308atanIC50of86nM.[3]Incellcyclestudies,cellgrowthwasinhibitedandcellsintheG1phasewereincreasedtwo-fold.[2]
Technicalinformation:
| ChemicalFormula: | C25H31N5O4 | |
| CAS#: | 938440-64-3 | |
| MolecularWeight: | 465.54 | |
| Purity: | >99% | |
| Appearance: | Yellow | |
| ChemicalName: | (5-(2-((2S,6R)-2,6-dimethylmorpholino)-4-morpholinopyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol | |
| Solubility: | Upto30mMinDMSO | |
| Synonyms: | KU-0063794,KU-63794,KU0063794,KU63794 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Malaguetal.,Thediscoveryandoptimisationofpyrido[2,3-d]pyrimidine-2,4-diaminesaspotentandselectiveinhibitorsofmTORkinase.Bioorg.Med.Chem.Lett.2009,19,5950-5953.PubmedID:19762236 |
| 2. | Garcia-Martinezetal.,Ku-0063794isaspecificinhibitorofthemammaliantargetofrapamycin(mTOR).Biochem.J.2009,421,29-42.PubmedID:19402821 |
| 3. | Liuetal.,Kinome-wideselectivityprofilingofATP-competitivemammaliantargetofrapamycin(mTOR)inhibitorsandcharacterizationoftheirbindingkinetics.J.Biol.Chem.2012,287(13),9742-9752.PubmedID:22223645 |
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