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Product Details

Acalabrutinib | Highly selective BTK inhibitor

Acalabrutinib (1420477-60-6) is a highly selective, potent (IC50 = 3 nM), and irreversible inhibitor of Bruton’s tyrosine kinase (BTK).1 Improved target selectivity (especially against TEC family kinases and EGFR) decreased the number of serious side effects observed with Ibrutinib.2 Acalabrutinib significantly inhibits BCR signaling, inhibits tumor proliferation, and reduces tumor burden.3 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.4

References/Citations

1) Wu et al. (2016), Acalabrutinnib (ACP-196): a second-generation BTK inhibitor; J. Hematol. Oncol. 9 21
2) Barf et al. (2017), Acalabrutinib (ACP-196): A covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile; J. Pharmacol. Exp. Ther. 363 240
3) Herman et al. (2017), The Bruton’s tyrosine kinase (BTK) inhibitor acalabrutinib demonstrates potent on-target effects and efficacy in two mouse models of chronic lymphocytic leukemia; Clin. Cancer Res. 23 2831
4) Weber et al. (2017), Bruton’s Tyrosine Kinase: An Emerging Key Player in Innate Immunity; Front. Immunol. 8 1454

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Catalog#  10-4806-0005

$45.00
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CAS:
1420477-60-6
Catalog Number:
10-4806
Alternate Name:
ACP-196
Activity:
Highly selective BTK inhibitor
Chemical Name:
4-[8-Amino-3-[(2S)-1-but-2-ynoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-pyridin-2-ylbenzamide
Molecular Weight:
465.52
Molecular Formula:
C26H23N7O2
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
Yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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