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203661 Bruton's Tyrosine Kinase Inhibitor III - CAS 936563-87-0 - Calbiochem

203661
  
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₂₅H₂₄N₆O₂936563-87-0
Description
Overview

This product has been discontinued.



A cell-permeable pyrrolopyridinyl-acryloyl compound that acts as a highly potent, selective, and irreversible inhibitor of BTK (IC50 = 720 pM), while affecting Lyn, Lck, and Itk activity only at much higher concentrations (IC50 = 14 nM, 97 nM, and 1.0 µM, respectively). Inhibits BTK-dependent PLC-γ1 phosphorylation and Ca2+ flux in human B cell line Ramos in vitro (IC50 = 14 nM and 40 nM, respectively) and is of excellent efficacy in a murine rheumatoid archritis model in vivo (>95% inhibition at 10 mg/kg/day, p.o.).

Catalogue Number203661
Brand Family Calbiochem®
Synonyms1-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, N-Acryloyl-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine
References
ReferencesPan, Z., et al. 2007. ChemMedchem. 2, 58.
Product Information
CAS number936563-87-0
FormWhite crystalline solid
Hill FormulaC₂₅H₂₄N₆O₂
Chemical formulaC₂₅H₂₄N₆O₂
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 Regulatory Review
Storage -20°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

Bruton's Tyrosine Kinase Inhibitor III - CAS 936563-87-0 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Bruton's Tyrosine Kinase Inhibitor III - CAS 936563-87-0 - Calbiochem Certificates of Analysis

TitleLot Number
203661

References

Reference overview
Pan, Z., et al. 2007. ChemMedchem. 2, 58.
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.

Revision19-May-2011 RFH
Synonyms1-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, N-Acryloyl-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine
DescriptionA cell-permeable pyrrolopyridinyl-acryloyl compound that acts as a highly potent, selective, and irreversible inhibitor of BTK (IC50 = 720 pM), while affecting Lyn, Lck, and Itk activity only at much higher concentrations (IC50 = 14 nM, 97 nM, and 1.0 µM, respectively). Inhibits BTK-dependent PLC-γ1 phosphorylation and Ca2+ flux in human B cell line Ramos in vitro (IC50 = 14 nM and 40 nM, respectively) and is of excellent efficacy in a murine rheumatoid archritis model in vivo (>95% inhibition at 10 mg/kg/day, p.o.).
FormWhite crystalline solid
Intert gas (Yes/No) Packaged under inert gas
CAS number936563-87-0
Chemical formulaC₂₅H₂₄N₆O₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (10 mg/ml) or Ethanol (5 mg/ml). Fresh DMSO is recommended.
Storage -20°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 Regulatory Review
ReferencesPan, Z., et al. 2007. ChemMedchem. 2, 58.