435300 LFM-A13 - CAS 62004-35-7 - Calbiochem

435300
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₁H₈Br₂N₂O₂ 62004-35-7

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      435300-5MG
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          Plastic ampoule 5 mg
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          Description
          OverviewA potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton’s Tyrosine Kinase (BTK; IC50 = 17.2 µM for human BTK in vitro and IC50 = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.
          Catalogue Number435300
          Brand Family Calbiochem®
          Synonymsα-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, BTK Inhibitor I, Bruton's Tyrosine Kinase Inhibitor I
          References
          ReferencesUckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.
          Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
          Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.
          Product Information
          CAS number62004-35-7
          ATP CompetitiveY
          FormLight brown solid
          Hill FormulaC₁₁H₈Br₂N₂O₂
          Chemical formulaC₁₁H₈Br₂N₂O₂
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetHuman Bruton's Tyrosine Kinase (BTK)
          Primary Target IC<sub>50</sub>17.2 µM for human BTK in vitro and 2.5 µM for recombinant BTK
          Purity≥97% by HPLC
          Physicochemical Information
          Cell permeableY
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          435300

          References

          Reference overview
          Uckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.
          Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
          Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.

          Citations

          Title
        • Sarah L Doyle, Caroline A Jefferies and Luke A O'Neill. (2005) Bruton's tyrosine kinase is involved in p65-mediated transactivation and phosphorylation of p65 on serine 536 during NF-B activation by LPS. Journal of Biological Chemistry 280, 23496-23501.
        • 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.

          Revision12-January-2010 RFH
          Synonymsα-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, BTK Inhibitor I, Bruton's Tyrosine Kinase Inhibitor I
          DescriptionA potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton's tyrosine kinase (BTK; IC50 = 17.2 µM for human BTK in vitro and IC50 = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.
          FormLight brown solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number62004-35-7
          Chemical formulaC₁₁H₈Br₂N₂O₂
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (200 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
          ReferencesUckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.
          Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
          Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.
          Citation
        • Sarah L Doyle, Caroline A Jefferies and Luke A O'Neill. (2005) Bruton's tyrosine kinase is involved in p65-mediated transactivation and phosphorylation of p65 on serine 536 during NF-B activation by LPS. Journal of Biological Chemistry 280, 23496-23501.