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218719 Casein Kinase I Inhibitor III, PF-4800567 - CAS 1188296-52-7 - Calbiochem

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CAS #Empirical Formula
1188296-52-7C₁₇H₁₈ClN₅O₂

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218719-5MG
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      Description
      OverviewA cell-permeable pyrazolopyrimidinylamino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKIε with ~22-fold greater potency over CKIδ (IC50 = 32 and 711 nM, respectively) and displays excellent selectivity among 50-kinases, with the only exception of EGFR (69% inhibition at 1 µM). Shown to preferentially block PER3 (PERIOD3) nuclear translocation in COS7-GFP-PER3-CKIε cells over CKIδ-transfected cells (IC50 = 0.13 and 2.65 µM, respectively), and PER2 degradation in COS7-GFP-PER2-CKIε cells. Unlike Casein Kinase I Inhibitor II, PF-670462 (Cat. No. 218716), PF-4800567 exerts only marginal effect on circadian clock under similar conditions.
      Catalogue Number218719
      Brand Family Calbiochem®
      Synonyms3-(3-Chlorophenoxymethyl)-1-(tetrahydropyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine, HCl, CKI Inhibitor III, PF-4800567
      References
      ReferencesMeng, Q.J., et al. 2010. Proc. Natl. Acad. Sci. USA 24, 15240.
      Etchegaray, J.P., et al. 2010. PLoS One 5, e10303.
      Walton, K.M., et al. 2009. J. Pharmacol. Exp. Ther. 330, 430.
      Badura, L., et al. 2007. J. Pharmacol. Exp. Ther. 322, 730.
      Product Information
      CAS number1188296-52-7
      FormBeige solid
      Hill FormulaC₁₇H₁₈ClN₅O₂
      Chemical formulaC₁₇H₁₈ClN₅O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥99% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      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). 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
      Global Trade Item Number
      Référence GTIN
      218719-5MG 04055977218947

      Documentation

      Casein Kinase I Inhibitor III, PF-4800567 - CAS 1188296-52-7 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Casein Kinase I Inhibitor III, PF-4800567 - CAS 1188296-52-7 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      218719

      Références bibliographiques

      Aperçu de la référence bibliographique
      Meng, Q.J., et al. 2010. Proc. Natl. Acad. Sci. USA 24, 15240.
      Etchegaray, J.P., et al. 2010. PLoS One 5, e10303.
      Walton, K.M., et al. 2009. J. Pharmacol. Exp. Ther. 330, 430.
      Badura, L., et al. 2007. J. Pharmacol. Exp. Ther. 322, 730.
      Fiche technique

      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.

      Revision20-July-2012 JSW
      Synonyms3-(3-Chlorophenoxymethyl)-1-(tetrahydropyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine, HCl, CKI Inhibitor III, PF-4800567
      DescriptionA cell-permeable pyrazolopyrimidinylamino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKIε with ~22-fold greater potency over CKIδ (IC50 = 32 and 711 nM, respectively) and displays excellent selectivity among 50-kinases, with the only exception of EGFR (69% inhibition at 1 µM). Shown to preferentially block PER3 (PERIOD3) nuclear translocation in COS7-GFP-PER3-CKIε cells over CKIδ-transfected cells (IC50 = 0.13 and 2.65 µM, respectively), and PER2 degradation in COS7-GFP-PER2-CKIε cells. Unlike Casein Kinase I Inhibitor II, PF-670462 (Cat. No. 218716), PF-4800567 exerts only marginal effect on circadian clock under similar conditions.
      FormBeige solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1188296-52-7
      Chemical formulaC₁₇H₁₈ClN₅O₂
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesMeng, Q.J., et al. 2010. Proc. Natl. Acad. Sci. USA 24, 15240.
      Etchegaray, J.P., et al. 2010. PLoS One 5, e10303.
      Walton, K.M., et al. 2009. J. Pharmacol. Exp. Ther. 330, 430.
      Badura, L., et al. 2007. J. Pharmacol. Exp. Ther. 322, 730.