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

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₁₇H₁₃BrClF₂IN₂O₂ 212631-67-9

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444967-5MG
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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 SDS

      Title

      Safety Data Sheet (SDS) 

      MEK1/2 Inhibitor IV - CAS 212631-67-9 - Calbiochem Certificates of Analysis

      TitleLot Number
      444967

      References

      Reference overview
      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.
      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.

      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.