ACP-5862 |
| رقم الكتالوجGC39541 |
ACP-5862 هو مستقلب رئيسي نشط ، متداول ، pyrrolidine مفتوح الحلقة من Acalabrutinib مع IC50 من 5.0 نانومتر لبروتون تيروزين كيناز (BTK)ACP ‐ 5862 هو معطل ضعيف يعتمد على الوقت لـ CYP3A4 و CYP2C8Acalabrutinib هو مثبط BTK نشط عن طريق الفم ، لا رجعة فيه ، وانتقائي للغاية ، مع IC 50 من 3 نانومتر و EC50 من 8 نانومتر
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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