KU-0063794
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MedKoo CAT#: 205776

CAS#: 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)


Chemical Structure

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KU-0063794
CAS# 938440-64-3

Theoretical Analysis

MedKoo Cat#: 205776
Name: KU-0063794
CAS#: 938440-64-3
Chemical Formula: C25H31N5O4
Exact Mass: 465.2376
Molecular Weight: 465.54474
Elemental Analysis: C, 64.50; H, 6.71; N, 15.04; O, 13.75

Price and Availability

Size Price Availability Quantity
25.0mg USD 150.0 2 Weeks
50.0mg USD 250.0 2 Weeks
100.0mg USD 450.0 2 Weeks
200.0mg USD 850.0 2 Weeks
500.0mg USD 1650.0 2 Weeks
1.0g USD 2950.0 2 Weeks
2.0g USD 4850.0 2 Weeks
5.0g USD 7650.0 2 Weeks
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Synonym: KU0063794; KU-0063794; KU 0063794; Ku0063794; Ku 0063794; Ku-0063794; KU63794; KU 63794; KU-63794.

IUPAC/Chemical Name: (5-(2-((2R,6S)-2,6-dimethylmorpholino)-4-morpholinopyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol

InChi Key: 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 Code: OCC1=CC(C2=NC3=NC(N4C[C@@H](C)O[C@@H](C)C4)=NC(N5CCOCC5)=C3C=C2)=CC=C1OC

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 465.54474 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.

Recalculate based on batch purity %
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

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1: Fan QW, Weiss WA. Inhibition of PI3K-Akt-mTOR signaling in glioblastoma by mTORC1/2 inhibitors. Methods Mol Biol. 2012;821:349-59. PubMed PMID: 22125077.

2: 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.

3: 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.

4: 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.

5: Sturgill TW, Hall MN. Activating mutations in TOR are in similar structures as oncogenic mutations in PI3KCalpha. ACS Chem Biol. 2009 Dec 18;4(12):999-1015. PubMed PMID: 19902965; PubMed Central PMCID: PMC2796128.

6: 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.

7: 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.
  



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