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217696 Cdk1 Inhibitor, CGP74514A - CAS 190654-01-4 - Calbiochem

217696
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
190654-01-4C₁₉H₂₄ClN₇

Products

Catalogue NumberPackaging Qty/Pack
217696-5MG Plastic ampoule 5 mg
Description
OverviewA cell-permeable and ATP competitive 2,6,9-substituted purine derivative that acts as a potent, selective inhibitor of Cdk1/cyclin B (IC50 = 25 nM). Reported to affect the activities of other kinases only at much higher concentrations (IC50 = 6.1 µM, 125 µM, and > 10 µM for PKCα, PKA, and EGFR, respectively). Shown to induce mitochondrial damage and apoptosis (≥ 3 µM) in several human leukemia cell lines. At lower concentrations (~1 µM), an initial G2M cell cycle arrest was observed in U937 cells, which eventually lead to apoptosis.
Catalogue Number217696
Brand Family Calbiochem®
SynonymsCGP74514A, N-(cis-2-Aminocyclohexyl)-N-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine
References
ReferencesYu. C., et al. 2003. Cancer Res. 63, 1822.
Dai, Y., et al. 2002. Cell Cycle 1, 143.
Imbach, P., et al. 1999. Bioorg. Med. Chem. Lett. 9, 91.
Product Information
CAS number190654-01-4
ATP CompetitiveY
DeclarationSold under license from Novartis Pharma AG.
FormOff-white solid
Hill FormulaC₁₉H₂₄ClN₇
Chemical formulaC₁₉H₂₄ClN₇
ReversibleN
Structure formula ImageStructure formula Image
Applications
Biological Information
Primary TargetCdk1/cyclin B
Primary Target IC<sub>50</sub>25 nM against Cdk1/cyclin B
Purity≥ 95% by HPLC
Physicochemical Information
Cell permeableY
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 Irritant
Storage -20°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
217696-5MG 04055977202328

Documentation

Cdk1 Inhibitor, CGP74514A - CAS 190654-01-4 - Calbiochem Certificates of Analysis

TitleLot Number
217696

References

Reference overview
Yu. C., et al. 2003. Cancer Res. 63, 1822.
Dai, Y., et al. 2002. Cell Cycle 1, 143.
Imbach, P., et al. 1999. Bioorg. Med. Chem. Lett. 9, 91.
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.

Revision16-December-2009 RFH
SynonymsCGP74514A, N-(cis-2-Aminocyclohexyl)-N-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine
DescriptionA cell-permeable, potent, reversible, ATP-competitive and selective inhibitor of Cdk1/cyclin B (IC50 = 25 nM). Affects the activities of other kinases only at higher concentrations (IC50 = 6.1 µM for PKCα, 125 µM for PKA, and >10 µM for EGFR). Also reported to induce mitochondrial damage and apoptosis in several human leukemia cell lines (>3 µM). At lower concentrations (~1 µM) an initial G2M cell cycle arrest and eventual apoptosis has been reported to occur in U937 cells.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number190654-01-4
Chemical formulaC₁₉H₂₄ClN₇
Structure formulaStructure formula
Purity≥ 95% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
-20°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 Irritant
ReferencesYu. C., et al. 2003. Cancer Res. 63, 1822.
Dai, Y., et al. 2002. Cell Cycle 1, 143.
Imbach, P., et al. 1999. Bioorg. Med. Chem. Lett. 9, 91.