217692 | CDC25 Phosphatase Inhibitor II, NSC 663284 - CAS 383907-43-5 - Calbiochem

217692
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₅H₁₆ClN₃O₃ 383907-43-5

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      217692-5MG
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          Plastic ampoule 5 mg
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          Description
          OverviewA cell-permeable 7-substituted quinolinedione compound that displays antiproliferative properties. Acts as a potent, irreversible and mixed competitive inhibitor of the CDC25 phosphatase family (Ki = 29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; IC50 = 210 nM for CDC25B2) and displays nearly 20- and 450-fold greater selectivity for the CDC252 phosphatases over VHR and PTP1B (IC50 = 4.0 µM and > 100 µM, respectively). Reported to arrest cell cycle progression, inhibit Cdk dephosphorylation and delay tumor growth (IC50 = ~1.5 µM in NCI-60 tumor cell panel). Shown to modify CDC25A catalytic domain and to block cellular ERK dephosphorylation in HeLa-CDC25A cells.
          Catalogue Number217692
          Brand Family Calbiochem®
          Synonyms6-Chloro-7-(2-morpholin-4-yl-ethylamino)quinoline-5,8-dione, DA3003-1, PTP Inhibitor XXI, VHR Inhibitor II
          References
          ReferencesChao, J. I., et al. 2004. J. Biol. Chem. 279, 20267.
          Han, Y., et al. 2004. J. Pharmacol. Exp. Ther. 309, 64.
          Pu, L., et al. 2002. J. Biol. Chem. 277, 46877.
          Lazo, J.S., et al. 2001. J. Med. Chem. 44, 4042.
          Product Information
          CAS number383907-43-5
          ATP CompetitiveN
          FormRed solid
          Hill FormulaC₁₅H₁₆ClN₃O₃
          Chemical formulaC₁₅H₁₆ClN₃O₃
          ReversibleN
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetCD25A
          Primary Target K<sub>i</sub>29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; 210 nM for CDC25B2
          Purity≥98% 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 Carcinogenic / Teratogenic
          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). DMSO stock solutions are stable for up to 1 month at -20°C. Ethanol 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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          217692

          References

          Reference overview
          Chao, J. I., et al. 2004. J. Biol. Chem. 279, 20267.
          Han, Y., et al. 2004. J. Pharmacol. Exp. Ther. 309, 64.
          Pu, L., et al. 2002. J. Biol. Chem. 277, 46877.
          Lazo, J.S., et al. 2001. J. Med. Chem. 44, 4042.
          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.

          Revision23-November-2010 JSW
          Synonyms6-Chloro-7-(2-morpholin-4-yl-ethylamino)quinoline-5,8-dione, DA3003-1, PTP Inhibitor XXI, VHR Inhibitor II
          DescriptionA cell-permable, potent, irreversible, and competitive inhibitor of the Cdc25 phosphatase family (Ki = 29 nM, 95 nM, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively) with anti-proliferative properties. Displays nearly 20- and 450-fold greater selectivity over VHR and PTP1B (IC50 = 4.0 µM and > 100 µM, respectively). Reported to arrest cell cycle progression, inhibit Cdk dephosphorylation, and delay tumor growth (mean IC50 = 1.5 µM in NCI-60 tumor cell panel). Also shown to block ERK dephosphorylation caused by ectopic Cdc25A expression.
          FormRed solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number383907-43-5
          Chemical formulaC₁₅H₁₆ClN₃O₃
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (5 mg/ml) or Ethanol (5 mg/ml). Use only fresh, anhydrous DMSO.
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 1 month at -20°C. Ethanol stock solutions are stable for up to 6 months at -20°C.
          Toxicity Carcinogenic / Teratogenic
          ReferencesChao, J. I., et al. 2004. J. Biol. Chem. 279, 20267.
          Han, Y., et al. 2004. J. Pharmacol. Exp. Ther. 309, 64.
          Pu, L., et al. 2002. J. Biol. Chem. 277, 46877.
          Lazo, J.S., et al. 2001. J. Med. Chem. 44, 4042.