Acalabrutinib, Highly selective BTK inhibitor (TBI4806)

Description

Product Details

Formal Name: 4-[8-Amino-3-[(2S)-1-but-2-ynoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-pyridin-2-ylbenzamide

Alternate Names: ACP-196

Molecular Formula: C₂₆H₂₃N₇O₂

Formula Weight: 465.52

CAS Number: 1420477-60-6

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Highly selective BTK inhibitor

Functions

Acalabrutinib (1420477-60-6) is a highly selective, potent (IC50 = 3nM), and irreversible inhibitor of Bruton’s tyrosine kinase (BTK). Improved target selectivity (especially against TEC family kinases and EGFR) decreased the number of serious side effects observed with Ibrutinib. Acalabrutinib significantly inhibits BCR signaling, inhibits tumor proliferation, and reduces tumor burden. Clinically useful agent for treating B-cell cancers. BTK has also been shown to have a role in modulating the innate immune system, especially in dendritic cells and macrophages, suggesting a possible role in immunotherapy.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.