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

217696
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₁₉H₂₄ClN₇190654-01-4

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217696-5MG
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      Plastic ampoule 5 mg
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      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

      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 -20°C
      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
      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.