ACP-5862 是 Acalabrutinib 的主要活性的，循环的，吡咯烷开环代谢产物，对于 Bruton 酪氨酸激酶 (BTK) 的 IC50 为 5.0 nM。Acalabrutinib 是一种口服有效的，选择性的 BTK 抑制剂，IC50 和 EC50 分别为 3 nM 和 8 nM。
货号:ajcx16822
CAS:2230757-47-6
分子式:C26H23N7O3
分子量：481.51
溶解度:DMSO: 250 mg/mL (519.20 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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)[1]. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM[2].

[1]. Podoll T, et al. Bioavailability, Biotransformation, and Excretion of the Covalent Bruton Tyrosine Kinase Inhibitor Acalabrutinib in Rats, Dogs, and Humans. Drug Metab Dispos. 2019 Feb;47(2):145-154. [2]. Herman SE, et al. The Bruton's tyrosine kinase (BTK) inhibitor acalabrutinib demonstrates potent on-target effects and efficacy in two mouse models of chronic lymphocytic leukemia. Clin Cancer Res. 2016 Nov 30