ACP-5862 |
Catalog No.GC39541 |
ACP-5862는 BTK(Bruton tyrosine kinase)에 대한 IC50이 5.0nM인 Acalabrutinib의 주요 활성 순환 피롤리딘 개환 대사산물입니다. ACP-5862는 CYP3A4 및 CYP2C8의 약한 시간 의존적 불활성화제입니다. 아칼라브루티닙은 IC50이 3nM이고 EC50이 8nM인 경구 활성, 비가역적, 고도로 선택적인 BTK 억제제입니다.
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Cas No.: 2230757-47-6
Sample solution is provided at 25 µL, 10mM.
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
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