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

217692
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Overview

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Key Spec Table

Empirical FormulaCAS #
C₁₅H₁₆ClN₃O₃383907-43-5

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217692-5MG
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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
      Quality LevelMQ100
      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

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

      Title

      Safety Data Sheet (SDS) 

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