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Acalabrutinib

Chemical Structure : Acalabrutinib

CAS No.: 1420477-60-6

Acalabrutinib (ACP-196, APC196)

Catalog No.: PC-45383Not For Human Use, Lab Use Only.

Acalabrutinib (ACP-196) is a potent, irreversible, covalent second-generation BTK inhibitor with IC50 of 3 nM.

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Biological Activity

Acalabrutinib (ACP-196) is a potent, irreversible, covalent second-generation BTK inhibitor with IC50 of 3 nM.
Acalabrutinib (ACP-196) is more potent and selective than ibrutinib, and does not inhibit EGFR, Itk or Txk.
Acalabrutinib (ACP-196) inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells.
Acalabrutinib (ACP-196) inhibits anti-IgM-induced CD86 expression in CD19+ splenocytes with an ED50 of 0.34 mg/kg in mice.
Acalabrutinib (ACP-196) has promising safety and efficacy profiles for CLL treatment; orally active.

Physicochemical Properties

M.Wt 465.5065
Formula C26H23N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 31 mg/mL

Chemical Name/SMILES

Benzamide, 4-[8-amino-3-[(2S)-1-(1-oxo-2-butyn-1-yl)-2-pyrrolidinyl]imidazo[1,5-a]pyrazin-1-yl]-N-2-pyridinyl-

References

1. Byrd JC, et al. N Engl J Med. 2016 Jan 28;374(4):323-32.

2. Herman SEM, et al. Clin Cancer Res. 2017 Jul 15;23(14):3734-3743.

3. Niemann CU, et al. Clin Cancer Res. 2017 Jun 23. pii: clincanres.0650.2017.

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