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203661-M

Sigma-Aldrich

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

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C25H24N6O2
CAS Number:
936563-87-0
Molecular Weight:
440.50
UNSPSC Code:
12352200

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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)

Storage Class Code

10-13 - German Storage Class 10 to 13

Certificates of Analysis (COA)

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