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218716 Casein Kinase I Inhibitor II, PF-670462 - CAS 950912-80-8 - Calbiochem

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Synonyme: 4-(3-Cyclohexyl-5-(4-fluorophenyl)-3H-imidazol-4-yl)-pyrimidin-2-ylamine, 2HCl

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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      950912-80-8C₁₉H₂₀FN₅ • 2HCl
      Description
      Overview

      This product has been discontinued.



      A cell-permeable tri-substituted imidazole compound that acts as a potent and reversible inhibitor of casein kinase Iε/δ (IC50 = 7.7 and 14 nM, respectively) with modest to excellent selectivity over EGFR and p38 MAPK (IC50 = 150 and 190 nM, respectively) and over 43 related kinases (IC50 > 0.3 to 30 µM), and a panel containing 116-receptors, transporters and other enzymes. Shown to inhibit PER3 nuclear translocation in GFP-PER3 and CKIε-cotransfected COS7 cells (EC50 = 290 nM), and induce phase delays in circadian rhythms of monkeys & rats model (10 - 100 mg, s.c.); further, attenuate the locomotor stimulant response to methamphetamine.
      Catalogue Number218716
      Brand Family Calbiochem®
      Synonyms4-(3-Cyclohexyl-5-(4-fluorophenyl)-3H-imidazol-4-yl)-pyrimidin-2-ylamine, 2HCl
      References
      ReferencesBryant, C.D., et al. 2009. Psychopharmacology 203, 703.
      Sprouse, J., et al. 2009. Psychopharmacology 204, 735.
      Badura, L., et al. 2007. J. Pharmacol. Exp. Ther. 322, 730.
      Product Information
      CAS number950912-80-8
      FormOff-white solid
      Hill FormulaC₁₉H₂₀FN₅ • 2HCl
      Chemical formulaC₁₉H₂₀FN₅ • 2HCl
      Hygroscopic Hygroscopic
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      S PhraseS: 22-24/25-36/37/39

      Do not breathe dust.
      Avoid contact with skin and eyes.
      Wear suitable protective clothing, gloves and eye/face protection.
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsSoluble in DMSO (< 100 mM) or H2O ( < 100 mM); aliquot & store at -20*C; stable for 6 months. Most likely to compete with ATP.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      218716 0

      Documentation

      Casein Kinase I Inhibitor II, PF-670462 - CAS 950912-80-8 - Calbiochem Analysenzertifikate

      TitelChargennummer
      218716

      Literatur

      Übersicht
      Bryant, C.D., et al. 2009. Psychopharmacology 203, 703.
      Sprouse, J., et al. 2009. Psychopharmacology 204, 735.
      Badura, L., et al. 2007. J. Pharmacol. Exp. Ther. 322, 730.