203661-M
Bruton′s Tyrosine Kinase Inhibitor III - CAS 936563-87-0 - Calbiochem
别名:
Bruton′s Tyrosine Kinase Inhibitor III - CAS 936563-87-0 - Calbiochem, 1-(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
description
The Bruton′s Tyrosine Kinase Inhibitor III, also referenced under CAS 936563-87-0, controls the biological activity of Bruton′s Tyrosine Kinase.
assay
≥98% (HPLC)
form
crystalline solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 10 mg/mL (Fresh DMSO is recommended.), ethanol: 5 mg/mL
storage temp.
−20°C
General description
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.).
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Pan, Z., et al. 2007. ChemMedchem.2, 58.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
存储类别
10-13 - German Storage Class 10 to 13
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