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219494 Cdk/CKI Inhibitor, (R)-DRF053 - CAS 1186647-87-9 - Calbiochem

The Cdk/CKI Inhibitor, (R)-DRF053, also referenced under CAS 1186647-87-9, controls the biological activity of Cdk/CKI. 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: 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(3-(2-pyridyl)phenylamino)-9-isopropylpurine, hydrate

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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1186647-87-9C₂₃H₂₇N₇O • H₂O
Description
OverviewA cell-permeable ATP-binding pocket-targeting (R)-Roscovitine (Cat. Nos. 550360 & 550364) derivative that is more potent than Roscovitine in inhibiting CDK1,CDK5, and CK1 activity (IC50 = 220,80,14 vs. 350, 200, 2300 nM, respectively), while maintaining selectivity against GSK-3α/β (IC50 = 4.1 µM). The CDK/CK1 dual-specificity nature of (R)-DRF053 most likely accounts for its superior activity to that of (R)-Roscovitine against β40 production from APP-expressing N2A cells (90% vs. 50% inhibition wtih 100 µM respective compound).
Catalogue Number219494
Brand Family Calbiochem®
Synonyms2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(3-(2-pyridyl)phenylamino)-9-isopropylpurine, hydrate
References
ReferencesOumata, N., et al. J. Med. Chem. 51, 5229.
Bettayeb, K., et al. 2008. Oncogene 27, 5797.
Product Information
CAS number1186647-87-9
FormPale yellow solid
Hill FormulaC₂₃H₂₇N₇O • H₂O
Chemical formulaC₂₃H₂₇N₇O • H₂O
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% 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 6 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
219494 0

Documentation

Cdk/CKI Inhibitor, (R)-DRF053 - CAS 1186647-87-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Cdk/CKI Inhibitor, (R)-DRF053 - CAS 1186647-87-9 - Calbiochem Certificates of Analysis

TitleLot Number
219494

References

Reference overview
Oumata, N., et al. J. Med. Chem. 51, 5229.
Bettayeb, K., et al. 2008. Oncogene 27, 5797.
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-March-2011 RFH
Synonyms2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(3-(2-pyridyl)phenylamino)-9-isopropylpurine, hydrate
DescriptionA cell-permeable ATP-binding pocket-targeting (R)-Roscovitine (Cat. Nos. 550360 & 550364) derivative that is more potent than Roscovitine in inhibiting CDK1/CDK5/CK1 activity (IC50 = 220/80/14 vs. 350/200/2300 nM, respectively), while maintaining selectivity against GSK-3α/β (IC50 = 4.1 µM). The CDK/CK1 dual-specificity nature of (R)-DRF053 most likely accounts for its superior activity to that of (R)-Roscovitine against β40 production from APP-expressing N2A cells (90% vs. 50% inhibition wtih100 µM respective compound).
FormPale yellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1186647-87-9
Chemical formulaC₂₃H₂₇N₇O • H₂O
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 mg/ml) or Ethanol (30 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 6 months at -20°C.
Toxicity Standard Handling
ReferencesOumata, N., et al. J. Med. Chem. 51, 5229.
Bettayeb, K., et al. 2008. Oncogene 27, 5797.