Acalabrutinib Metabolite 27
Acalabrutinib Metabolite 27 Basic information
- Product Name:
- Acalabrutinib Metabolite 27
- Synonyms:
-
- Acalabrutinib Metabolite 27
- Acalabrutinib?active?metabolite?M27
- 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
- ACP-5862
- Acalabrutinib Impurity 1
- 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
- Acalabrutinib Metabolite 27 (ACP-5862)
- CAS:
- 2230757-47-6
- MF:
- C26H23N7O3
- MW:
- 481.51
- Mol File:
- 2230757-47-6.mol
Acalabrutinib Metabolite 27 Chemical Properties
- Density
- 1.34±0.1 g/cm3(Predicted)
- pka
- 11.35±0.70(Predicted)
- form
- Solid
- color
- White to off-white
Acalabrutinib Metabolite 27 Usage And Synthesis
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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