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203881 CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem

A cell-permeable (R)-DRF053 analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor.

CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (R)-CR8, Cdk7 Inhibitor VII

203881
  
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

CAS #Empirical Formula
294646-77-8C₂₄H₂₉N₇O
Description
OverviewA cell-permeable (R)-DRF053 (Cat. No. 219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC50 = 0.09, 0.072, 0.041, 0.11, 1.10, 0.18, and 0.40 µM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK7/H, CDK9/T, and CK1δ/ε, respectively). As is the case with (R)-DRF053, (R)-CR8 inhibits CDK/CK1 more effectively than (R)-Roscovitine (Cat. Nos. 550360 & 550364), while maintaining similar selectivity profile over other types of kinases (IC50 = 3.6, 3.6, and 12.0 µM against Dyrk1A, Erk2, and GSK-3α/β, respectively). Both the (R)-CR8 and (S)-enantiomer (Cat. No. 203882) are much more effective than (R)-Roscovitine in apoptosis induction in cell cultures.
Catalogue Number203881
Brand Family Calbiochem®
Synonyms2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (R)-CR8, Cdk7 Inhibitor VII
References
ReferencesOumata, N., et al. J. Med. Chem. 51, 5229.
Bettayeb, K., et al. 2008. Oncogene 27, 5797.
Product Information
CAS number294646-77-8
FormOff-white solid
Hill FormulaC₂₄H₂₉N₇O
Chemical formulaC₂₄H₂₉N₇O
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% 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
Katalógusszám GTIN
203881 0

Documentation

CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem Certificates of Analysis

TitleLot Number
203881

References

Hivatkozások áttekintése
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-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (R)-CR8, Cdk7 Inhibitor VII
DescriptionA cell-permeable (R)-DRF053 (Cat. No. 219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC50 = 0.09, 0.072, 0.041, 0.11, 1.10, 0.18, and 0.40 µM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK7/H, CDK9/T, and CK1δ/ε, respectively). As is the case with (R)-DRF053, (R)-CR8 inhibits CDK/CK1 more effectively than (R)-Roscovitine (Cat. Nos. 550360 & 550364), while maintaining similar selectivity profile over other types of kinases (IC50 = 3.6, 3.6, and 12.0 µM against Dyrk1A, Erk2, and GSK-3α/β, respectively). Both (R)-CR8 & its (S)-enantiomer (Cat. No. 203882) are much more effective than (R)-Roscovitine in apoptosis induction in cell cultures.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number294646-77-8
Chemical formulaC₂₄H₂₉N₇O
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (50 mg/ml) or Ethanol (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 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.