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475990 mTOR Inhibitor IV, Ku-63794 - CAS 938440-64-3 - Calbiochem

The mTOR Inhibitor IV, Ku-63794, also referenced under CAS 938440-64-3, controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: rel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol, Ku-0063794, mTOR Inhibitor IV, Ku-63794

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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
938440-64-3C₂₅H₃₁N₅O₄

Products

Catalogue NumberPackaging Qty/Pack
475990-5MGCN Glass bottle 5 mg
Description
OverviewA cell-permeable pyrido-pyrimidine compound that acts as a highly selective and potent inhibitor against both mTORC1 & mTORC2 (IC50 = ~10 nM against mTOR activity in raptor or rictor immunoprecipitate from HEK293 with 100 µM ATP), with much reduced potency against MKK1 and PI 3-Kα (IC50 ~9 µM) and little or no activity toward more than 200 other protein and lipid kinases, including Akt, ATR, DNA-PK, PDK1, and PI 3-Kβ/γ/δ. Shown to effectively inhibit cellular mTOR phosphorylation on Ser2448/2481 as well as the phosphorylation and activation of mTORC1/2 downstream effector molecules such as Akt, S6K, 4E-BP1, but not RSK or Erk1/2, kinases that are not regulated by mTOR. Although Ku-63794 is shown not to affect IGF-1-induced Akt phosphorylation on Ser308 by PDK1 in mTORC2 knockout MEF cultures, Ku-63794 treatment of mTORC2-expressing MEF cells is shown to inhibit IGF-1-induced Akt Ser308 phosphorylation.
Catalogue Number475990
Brand Family Calbiochem®
Synonymsrel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol, Ku-0063794, mTOR Inhibitor IV, Ku-63794
References
ReferencesMalagu, K., et al. 2009. Bioorg. Med. Chem. Lett. 19, 5950.
Garcia-Martinez, J.M., et al. 2009. Biochem. J. 421, 29.
Product Information
CAS number938440-64-3
FormPale yellow solid
Hill FormulaC₂₅H₃₁N₅O₄
Chemical formulaC₂₅H₃₁N₅O₄
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
475990-5MGCN 04055977184426

Documentation

mTOR Inhibitor IV, Ku-63794 - CAS 938440-64-3 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

mTOR Inhibitor IV, Ku-63794 - CAS 938440-64-3 - Calbiochem Certificates of Analysis

TitleLot Number
475990

References

Reference overview
Malagu, K., et al. 2009. Bioorg. Med. Chem. Lett. 19, 5950.
Garcia-Martinez, J.M., et al. 2009. Biochem. J. 421, 29.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision31-August-2010 RFH
Synonymsrel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol, Ku-0063794, mTOR Inhibitor IV, Ku-63794
DescriptionA cell-permeable pyrido-pyrimidine compound that acts as a highly selective and potent inhibitor against both mTORC1 & mTORC2 (IC50 = ~10 nM against mTOR activity in raptor or rictor immunoprecipitate from HEK293 with 100 µM ATP), with much reduced potency against MKK1 and PI 3-Kα (IC50 ~9 µM) and little or no activity toward more than 200 other protein and lipid kinases, including Akt, ATR, DNA-PK, PDK1, and PI 3-Kβ/γ/δ. Shown to effectively inhibit cellular mTOR phosphorylation on Ser2448/2481 as well as the phosphorylation and activation of mTORC1/2 downstream effector molecules such as Akt, S6K, 4E-BP1, but not RSK or Erk1/2, kinases that are not regulated by mTOR. Although Ku-63794 is shown not to affect IGF-1-induced Akt phosphorylation on Ser308 by PDK1 in mTORC2 knockout MEF cultures, Ku-63794 treatment of mTORC2-expressing MEF cells is shown to inhibit IGF-1-induced Akt Ser308 phosphorylation.
FormPale yellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number938440-64-3
Chemical formulaC₂₅H₃₁N₅O₄
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (15 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesMalagu, K., et al. 2009. Bioorg. Med. Chem. Lett. 19, 5950.
Garcia-Martinez, J.M., et al. 2009. Biochem. J. 421, 29.