KU 0063794

Pricing Availability Delivery Time Qty
Cat.No. 3725 - KU 0063794 | C25H31N5O4 | CAS No. 938440-64-3
Description: Selective mTOR inhibitor
Chemical Name: rel-5-[2-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol
Purity: ≥97% (HPLC)
Datasheet
Citations (7)

Biological Activity

Selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2). Displays no activity at PI 3-kinase or 76 other kinases tested. Inhibits activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not RSK. Suppresses cell growth and induces G1 cell cycle arrest in vitro.

Licensing Information

Sold for research purposes only under agreement from KUDOS

Technical Data

M. Wt 465.54
Formula C25H31N5O4
Storage Store at RT
Purity ≥97% (HPLC)
CAS Number 938440-64-3
PubChem ID 16736978
InChI Key RFSMUFRPPYDYRD-CALCHBBNSA-N
Smiles OCC1=C(OC)C=CC(C3=NC2=NC(N5C[C@@H](C)O[C@@H](C)C5)=NC(N4CCOCC4)=C2C=C3)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 4.66 10

Preparing Stock Solutions

The following data is based on the product molecular weight 465.54. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.15 mL 10.74 mL 21.48 mL
5 mM 0.43 mL 2.15 mL 4.3 mL
10 mM 0.21 mL 1.07 mL 2.15 mL
50 mM 0.04 mL 0.21 mL 0.43 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Garcia-Martinez et al (2009) Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem.J. 421 29 PMID: 19402821


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Keywords: KU0063794 mammalian target of rapamycin inhibitors inhibits selective mTOR kinases suppresses cell growth mTOR

7 Citations for KU 0063794

Citations are publications that use Tocris products. Selected citations for KU 0063794 include:

Hukelmann et al (2016) The cytotoxic T cell proteome and its shaping by the kinase mTOR. J Biol Chem 17 104 PMID: 26551880

López-Cotarelo et al (2015) A novel MEK-ERK-AMPK signaling axis controls chemokine receptor CCR7-dependent survival in human mature dendritic cells. Proc Natl Acad Sci U S A 290 827 PMID: 25425646

Munson et al (2015) mTOR activates the VPS34-UVRAG complex to regulate autolysosomal tubulation and cell survival. Nat Immunol 34 2272 PMID: 26139536

Wang et al (2014) SynGAP regulates protein synthesis and homeostatic synaptic plasticity in developing cortical networks. PLoS One 8 e83941 PMID: 24391850

Fei et al (2013) Targeting mTOR to overcome epidermal growth factor receptor tyrosine kinase inhibitor resistance in non-small cell lung cancer cells. PLoS One 8 e69104 PMID: 23874880

Sengupta et al (2013) Regulation of OSR1 and the sodium, potassium, two chloride cotransporter by convergent signals. Free Radic Biol Med 110 18826 PMID: 24191005

Montané and Menand (2013) ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change. EMBO J 64 4361 PMID: 23963679


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