ACP-5862 |
| Catalog No.GC39541 |
L'ACP-5862 est un métabolite pyrrolidine actif, circulant et À cycle ouvert majeur de l'acalabrutinib avec une IC50 de 5,0 nM pour la Bruton tyrosine kinase (BTK). L'ACP‐5862 est un faible inactivateur dépendant du temps du CYP3A4 et du CYP2C8. L'acalabrutinib est un inhibiteur de BTK actif par voie orale, irréversible et hautement sélectif, avec une IC50 de 3 nM et une CE50 de 8 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2230757-47-6
Sample solution is provided at 25 µL, 10mM.
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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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