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Bruton's Tyrosine Kinase Inhibitor III
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
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.).
产品信息
Form White crystalline solid
Molar mass 440.5
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility DMSO or EtOH
Chemical formula C25H24N6O2
CAS number 936563-87-0
商店和运输信息
Storage -20°C
Ship Ambient Temperature Only
Regulatory Review |