506172 | p38 MAP Kinase Inhibitor X, BIRB 796 - CAS 285983-48-4 - Calbiochem

506172
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₃₁H₃₇N₅O₃ 285983-48-4

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      506172-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38α, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38α = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2α2 and c-Raf-1 only at much higher concentrations (IC50 = 98 nM and 1.4 µM, respectively) and displays little or no activity toward 10 other kinases (IC50 >20 µM). Shown to inhibit LPS-induced TNF-α production both in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84%; 30 mg/kg p.o.).
          Catalogue Number506172
          Brand Family Calbiochem®
          SynonymsDoramapimod, BIRB796, 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII
          References
          ReferencesLiu. Y. and Gray, N.S., 2006. Nat. Chem. Biol. 2, 358.
          Regan, J., et al. 2003. J. Med. Chem. 46, 4676.
          Pargellis, C., et al. 2002. Nat. Struct. Biol. 9, 268.
          Regan, J., et al. 2002. J. Med. Chem. 45, 2994.
          Product Information
          CAS number285983-48-4
          FormWhite solid
          Hill FormulaC₃₁H₃₇N₅O₃
          Chemical formulaC₃₁H₃₇N₅O₃
          Structure formula ImageStructure formula Image
          Applications
          Applicationp38 MAP Kinase Inhibitor X, BIRB 796, CAS 285983-48-4, is a cell-permeable, highly potent, slow binding, high affinity inhibitor of p38a (IC50 = 8 and 97 nM with or without 2 h preincubation).
          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 Regulatory Review
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          506172

          References

          Reference overview
          Liu. Y. and Gray, N.S., 2006. Nat. Chem. Biol. 2, 358.
          Regan, J., et al. 2003. J. Med. Chem. 46, 4676.
          Pargellis, C., et al. 2002. Nat. Struct. Biol. 9, 268.
          Regan, J., et al. 2002. J. Med. Chem. 45, 2994.
          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.

          Revision02-October-2012 JSW
          SynonymsDoramapimod, BIRB796, 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII
          DescriptionA cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38α, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38α = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2α2 and c-Raf-1 only at much higher concentrations (IC50 = 98 nM and 1.4 µM, respectively) and displays little or no activity toward 10 other kinases (IC50 >20 µM). Shown to inhibit LPS-induced TNF-α production in cultures in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84% and 63%, respectively, with oral dosage of 30 mg/kg and 10 mg/kg).
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number285983-48-4
          Chemical formulaC₃₁H₃₇N₅O₃
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (50 mg/ml; clear, colorless solution)
          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 6 months at -20°C.
          Toxicity Regulatory Review
          ReferencesLiu. Y. and Gray, N.S., 2006. Nat. Chem. Biol. 2, 358.
          Regan, J., et al. 2003. J. Med. Chem. 46, 4676.
          Pargellis, C., et al. 2002. Nat. Struct. Biol. 9, 268.
          Regan, J., et al. 2002. J. Med. Chem. 45, 2994.