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

217696
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₉H₂₄ClN₇ 190654-01-4

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.