ACP-5862 |
| カタログ番号GC39541 |
ACP-5862 は、ブルトン型チロシンキナーゼ (BTK) の IC50 が 5.0 nM である Acalabrutinib の主要な活性循環型ピロリジン開環代謝物です。 ACP-5862 は、CYP3A4 および CYP2C8 の弱い時間依存性不活化剤です。 Acalabrutinib は経口活性で不可逆的で選択性の高い BTK 阻害剤であり、IC50 は 3 nM、EC50 は 8 nM です。
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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