203881 Sigma-AldrichCR8, (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.
More>> A cell-permeable (R)-DRF053 analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor. Less<<Synonyms: 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (R)-CR8, Cdk7 Inhibitor VII
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Overview
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Key Spec Table
CAS # | Empirical Formula |
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294646-77-8 | C₂₄H₂₉N₇O |
Description | |
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Overview | A 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 Number | 203881 |
Brand Family | Calbiochem® |
Synonyms | 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (R)-CR8, Cdk7 Inhibitor VII |
References | |
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References | Oumata, N., et al. J. Med. Chem. 51, 5229. Bettayeb, K., et al. 2008. Oncogene 27, 5797. |
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CAS number | 294646-77-8 |
Form | Off-white solid |
Hill Formula | C₂₄H₂₉N₇O |
Chemical formula | C₂₄H₂₉N₇O |
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Quality Level | MQ100 |
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Purity | ≥97% by HPLC |
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Packaged under inert gas | Packaged under inert gas |
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Catalogue Number | GTIN |
203881 | 0 |
Documentation
CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem MSDS
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CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem Certificates of Analysis
Title | Lot Number |
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203881 |
References
Reference overview |
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Oumata, N., et al. J. Med. Chem. 51, 5229. Bettayeb, K., et al. 2008. Oncogene 27, 5797. |