Cofttek holdings limited

Akt &GSK-3

KU-0063794 (938440-64-3)

KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM; no effect on PI3Ks….

Not Intended for Therapeutic Use. For research use only.

CAS: 938440-64-3 Category

KU-0063794 (938440-64-3) Description:

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)

KU-0063794 (938440-64-3) Specifications:

Product Name KU-0063794
Synonym KU0063794; KU-0063794; KU 0063794; Ku0063794; Ku 0063794; Ku-0063794; KU63794; KU 63794; KU-63794.
Chemical Name (5-(2-((2R,6S)-2,6-dimethylmorpholino)-4-morpholinopyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 938440-64-3
Molecular Formula C25H31N5O4
Molecular Weight 465.54474
Monoisotopic Mass 465.2376 g/mol
MDL number MFCD11977741
InChIKey RFSMUFRPPYDYRD-CALCHBBNSA-N
InChi Code InChI=1S/C25H31N5O4/c1-16-13-30(14-17(2)34-16)25-27-23-20(24(28-25)29-8-10-33-11-9-29)5-6-21(26-23)18-4-7-22(32-3)19(12-18)15-31/h4-7,12,16-17,31H,8-11,13-15H2,1-3H3/t16-,17+
SMILES OCC1=CC(C2=NC3=NC(N4C[[email protected]@H](C)O[[email protected]@H](C)C4)=NC(N5CCOCC5)=C3C=C2)=CC=C1OC
Form Powder
Color White
Solubility  Soluble in DMSO, not soluble in water
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application KU-0063794 is a potent and selective mTOT inhibitor

 


=

RIDADR NONH for all modes of transport

References:

[1]. Case N, Thomas J, Sen B, Styner M, Xie Z, Galior K, Rubin J. Mechanical regulation of glycogen synthase kinase 3β (GSK3β) in mesenchymal stem cells is dependent on Akt protein serine 473 phosphorylation via mTORC2 protein. J Biol Chem. 2011 Nov 11;286(45):39450-6. Epub 2011 Sep 28. PubMed PMID: 21956113; PubMed Central PMCID: PMC3234768.

[2]. Dormond-Meuwly A, Roulin D, Dufour M, Benoit M, Demartines N, Dormond O. The inhibition of MAPK potentiates the anti-angiogenic efficacy of mTOR inhibitors. Biochem Biophys Res Commun. 2011 Apr 22;407(4):714-9. Epub 2011 Mar 23. PubMed PMID: 21439267.

[3]. Cheng J, Wang Y, Ma Y, Chan BT, Yang M, Liang A, Zhang L, Li H, Du J. The mechanical stress-activated serum-, glucocorticoid-regulated kinase 1 contributes to neointima formation in vein grafts. Circ Res. 2010 Nov 12;107(10):1265-74. Epub 2010 Sep 30. Erratum in: Circ Res. 2011 Jan 7;108(1):e1. PubMed PMID: 20884880.

[4]. Malagu K, Duggan H, Menear K, Hummersone M, Gomez S, Bailey C, Edwards P, Drzewiecki J, Leroux F, Quesada MJ, Hermann G, Maine S, Molyneaux CA, Le Gall A, Pullen J, Hickson I, Smith L, Maguire S, Martin N, Smith G, Pass M. 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 Oct 15;19(20):5950-3. Epub 2009 Aug 13. PubMed PMID: 19762236.

[5].García-Martínez JM, Moran J, Clarke RG, Gray A, Cosulich SC, Chresta CM, Alessi DR. Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem J. 2009 Jun 12;421(1):29-42. PubMed PMID: 19402821; PubMed Central PMCID: PMC2708931.

1 review for KU-0063794 (938440-64-3)

  1. Cofttek

    Never had such good experience before,The KU-0063794 (938440-64-3) is high purity,also customer service is pretty nice !gotta try!!

Add a review

Your email address will not be published. Required fields are marked *