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

A 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).

LFM-A13 - CAS 62004-35-7 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: α-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, BTK Inhibitor I, Bruton's Tyrosine Kinase Inhibitor I

Primary Target: Human Bruton's Tyrosine Kinase (BTK)
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
62004-35-7C₁₁H₈Br₂N₂O₂

Products

Catalogue NumberPackaging Qty/Pack
435300-5MGCN 塑膠安瓿;塑膠針藥瓶 5 mg
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
Quality LevelMQ100
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
Global Trade Item Number
Catalogue Number GTIN
435300-5MGCN 04055977210293

Documentation

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

Title

Safety Data Sheet (SDS) 

LFM-A13 - CAS 62004-35-7 - Calbiochem 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 Protect from light
    +2°C to +8°C
    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.
    		•