| Identification | Back Directory | [Name]
Acalabrutinib Metabolite 27 | [CAS]
2230757-47-6 | [Synonyms]
ACP-5862
Acalabrutinib Impurity 1
Acalabrutinib Metabolite 27
Acalabrutinib?active?metabolite?M27
Acalabrutinib Metabolite 27 (ACP-5862)
Acalabrutinib Metabolite 27 (Acalabrutinib Impurity 1)
4-(8-Amino-3-(4-(but-2-ynamido)butanoyl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide
4-[8-amino-3-[1-oxo-4-[(1-oxo-2-butyn-1-yl)amino]butyl]imidazo[1,5-a]pyrazin-1-yl]-N-2-pyridinyl-Benzamide
Benzamide, 4-[8-amino-3-[1-oxo-4-[(1-oxo-2-butyn-1-yl)amino]butyl]imidazo[1,5-a]pyrazin-1-yl]-N-2-pyridinyl-
Acalabrutinib Metabolite (M27) ACP-5862 D4Q: What is
Acalabrutinib Metabolite (M27) ACP-5862 D4 Q: What is the CAS Number of
Acalabrutinib Metabolite (M27) ACP-5862 D4 | [Molecular Formula]
C26H23N7O3 | [MDL Number]
MFCD32693908 | [MOL File]
2230757-47-6.mol | [Molecular Weight]
481.51 |
| Hazard Information | Back Directory | [Uses]
4-[8-Amino-3-[1-oxo-4-[(1-oxo-2-butyn-1-yl)amino]butyl]imidazo[1,5-a]pyrazin-1-yl]-N-2-pyridinyl-benzamide is a metabolite of Acalabrutinib (A115605) which is an experimental anti-cancer drug and a selective Bruton''s tyrosine kinase (BTK) inhibitor. This kinase transmits signals from B-cell Receptor (BCR), and thus any genetic BTK mutation causes B-Cell immunodeficiency. Therefore, BTK inhibitors targeting B-cell signaling has shown great promise for the treatment of chronic lymphocytic leukemia (CLL). | [in vivo]
Following a single oral dose of 100 mg Acalabrutinib, the half‐life of ACP‐5862 is 6.9 hours and the mean exposure is approximately twofold to threefold higher than that of Acalabrutinib[2].
ACP-5862 (M27) is the major single metabolite in the systemic circulation and accountes for 57.4% and 42.1% of the AUC0-t total radioactivity in male and female rat plasma, respectively. ACP-5862, the major human metabolite, is a relatively minor component in the systemic circulation and accountes for 6.1% and 8.1% of the AUC0-t total radioactivity in male and female dog plasma, respectively[1].
ACP-5862 (1 or 10 μM) has reversible protein binding of 98.6%, 99.8%, 94.3%, 98.6% in mouse, rat, dog, and human plasma[1].
| [IC 50]
CYP2C8; CYP3A4 |
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