产品
编 号：F280221
分子式：C26H23N7O3
分子量：481.51
分子式：C26H23N7O3
分子量：481.51
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2230757-47-6
产品详情
生物活性：
ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.
体内研究：
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. 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. 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.
ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.
体内研究：
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. 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. 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.
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