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ACP-5862

Cat. No. M14321

All AbMole products are for research use only, cannot be used for human consumption.

ACP-5862 Structure

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Quality Control & Documentation
Biological Activity

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). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.

Chemical Information
Molecular Weight 481.51
CAS Number 2230757-47-6
Solubility (25°C) DMSO 150 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Helena Edlund, et al. Exposure-response analysis of acalabrutinib and its active metabolite, ACP-5862, in patients with B-cell malignancies

[2] Helena Edlund, et al. Improved characterization of the pharmacokinetics of acalabrutinib and its pharmacologically active metabolite, ACP-5862, in patients with B-cell malignancies and in healthy subjects using a population pharmacokinetic approach

[3] Qiong Liu, et al. ACP-5862 suppresses esophageal squamous cell carcinoma growth through inducing apoptosis via activation of endoplasmic reticulum stress and ROS production

[4] Zheli Jiang, et al. Simultaneous measurement of acalabrutinib, ibrutinib, and their metabolites in beagle dog plasma by UPLC-MS/MS and its application to a pharmacokinetic study

[5] Diansong Zhou, et al. Evaluation of the Drug-Drug Interaction Potential of Acalabrutinib and Its Active Metabolite, ACP-5862, Using a Physiologically-Based Pharmacokinetic Modeling Approach

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Keywords: ACP-5862 supplier, inhibitors, activators

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