444967 MEK1/2 Inhibitor IV - CAS 212631-67-9 - Calbiochem

444967
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      Replacement Information

      Tableau de caractéristiques principal

      Empirical FormulaCAS #
      C₁₇H₁₃BrClF₂IN₂O₂ 212631-67-9

      Prix & Disponibilité

      Référence DisponibilitéConditionnement Qté Prix Quantité
      444967-5MG
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      Disponibilité limitéeDisponibilité limitée
      En stock 
      Interrompu(e)
      Disponible en quantités limitées
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          5 mg
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          Description
          OverviewA cell-permeable, blood-brain barrier permeant, and orally active hydroxamate compound that is reported to inhibit MEK activity (IC50 = 10-100 nM) without competing against ATP or Erk binding and exhibit excellent selectivity over 27 other cellular kinases, including JNK, MAPK2/ERK2, SAPK2a, SAPK2b, SAPK3, and SAPK4 (IC50 > 10 µM). Shown to be superior to PD 98059 (Cat. Nos. 513000 and 513001) and U0126 (Cat. No. 662005) in suppressing Erk1/2 phosphorylation in Hep3B, HepG2, PLC, and SKHep human liver cancer cells (IC50 <0.1 µM) in vitro and effectively reduce Erk1/2 phosphorylation in hippocampal tissue in mice (ED50 <50 mg/kg, i.p.) in vivo. Both PD184161 and U0126 are shown to induce necrosis of several types of glucose-deprived cells via an indirect action on the F0 component of the mitochondrial F1F0-ATPase/synthase.
          Catalogue Number444967
          Brand Family Calbiochem®
          Synonyms2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-5-bromo-benzamide, PD184161, MEK Inhibitor IV
          References
          ReferencesYip-Schneider, M.T., et al. 2009. J. Pharmacol. Exp. Ther. 329, 1063.
          Duman, C.H., et al. 2007. Biol. Psychiatry 61, 661.
          Klein, P.J., et al. 2006. Neoplasia 8, 1.
          Thottassery, J.V., et al. 2004. Cancer Res. 64, 4637.
          Yung, H.W., et al. 2004. Biochem. Pharmacol. 68, 351.
          Product Information
          CAS number212631-67-9
          FormWhite solid
          Hill FormulaC₁₇H₁₃BrClF₂IN₂O₂
          Chemical formulaC₁₇H₁₃BrClF₂IN₂O₂
          Structure formula ImageStructure formula Image
          Quality LevelMQ100
          Applications
          Biological Information
          Purity≥98% 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 Ambient Temperature Only
          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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          MEK1/2 Inhibitor IV - CAS 212631-67-9 - Calbiochem FDS

          Titre

          Fiche de données de sécurité des matériaux (FDS) 

          MEK1/2 Inhibitor IV - CAS 212631-67-9 - Calbiochem Certificats d'analyse

          TitreNuméro de lot
          444967

          Références bibliographiques

          Aperçu de la référence bibliographique
          Yip-Schneider, M.T., et al. 2009. J. Pharmacol. Exp. Ther. 329, 1063.
          Duman, C.H., et al. 2007. Biol. Psychiatry 61, 661.
          Klein, P.J., et al. 2006. Neoplasia 8, 1.
          Thottassery, J.V., et al. 2004. Cancer Res. 64, 4637.
          Yung, H.W., et al. 2004. Biochem. Pharmacol. 68, 351.
          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.

          Revision15-July-2010 RFH
          Synonyms2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-5-bromo-benzamide, PD184161, MEK Inhibitor IV
          DescriptionA cell-permeable, blood-brain barrier permeant, and orally active hydroxamate compound that is reported to inhibit MEK activity (IC50 = 10-100 nM) without competing against ATP or Erk binding and exhibit excellent selectivity over 27 other cellular kinases, including JNK, MAPK2/ERK2, SAPK2a, SAPK2b, SAPK3, and SAPK4 (IC50 > 10 µM). Shown to be superior to PD 98059 (Cat. Nos. 513000 and 513001 and U0126 (Cat. No. 662005) in suppressing Erk1/2 phosphorylation in Hep3B, HepG2, PLC, and SKHep human liver cancer cells (IC50 <0.1 µM) in vitro and effectively reduce Erk1/2 phosphorylation in hippocampal tissue in mice (ED50 <50 mg/kg, i.p.) in vivo. Both PD184161 and U0126 are shown to induce necrosis of several types of glucose-deprived cells via an indirect action on the F0 component of the mitochondrial F1F0-ATPase/synthase.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number212631-67-9
          Chemical formulaC₁₇H₁₃BrClF₂IN₂O₂
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml) or Ethanol (5 mg/ml)
          Storage +2°C to +8°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 Standard Handling
          ReferencesYip-Schneider, M.T., et al. 2009. J. Pharmacol. Exp. Ther. 329, 1063.
          Duman, C.H., et al. 2007. Biol. Psychiatry 61, 661.
          Klein, P.J., et al. 2006. Neoplasia 8, 1.
          Thottassery, J.V., et al. 2004. Cancer Res. 64, 4637.
          Yung, H.W., et al. 2004. Biochem. Pharmacol. 68, 351.