Acalabrutinib Metabolite 27
- Product Name
- Acalabrutinib Metabolite 27
- CAS No.
- 2230757-47-6
- Chemical Name
- Acalabrutinib Metabolite 27
- Synonyms
- ACP-5862;ACP5862,ACP 5862;Acalabrutinib Impurity 1;Acalabrutinib Metabolite 27;Acalabrutinib Metabolite [AC-5862;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
- CBNumber
- CB15417707
- Molecular Formula
- C26H23N7O3
- Formula Weight
- 481.51
- MOL File
- 2230757-47-6.mol
Acalabrutinib Metabolite 27 Property
- Density
- 1.34±0.1 g/cm3(Predicted)
- pka
- 11.35±0.70(Predicted)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- A621885
- Product name
- 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
- Packaging
- 10mg
- Price
- $1540
- Updated
- 2021/12/16
- Product number
- CS-0111509
- Product name
- ACP-5862
- Purity
- 98.09%
- Packaging
- 50mg
- Price
- $2800
- Updated
- 2021/12/16
- Product number
- CS-0111509
- Product name
- ACP-5862
- Purity
- 98.09%
- Packaging
- 1mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- CS-0111509
- Product name
- ACP-5862
- Purity
- 98.09%
- Packaging
- 5mg
- Price
- $650
- Updated
- 2021/12/16
- Product number
- CS-0111509
- Product name
- ACP-5862
- Purity
- 98.09%
- Packaging
- 10mg
- Price
- $950
- Updated
- 2021/12/16
Acalabrutinib Metabolite 27 Chemical Properties,Usage,Production
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
Acalabrutinib Metabolite 27 Preparation Products And Raw materials
Raw materials
Preparation Products
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