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ACP-5862
$300 – $2,800
Products Details
Product Description
– 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[1][2].
Web ID
– HY-135334
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C26H23N7O3
References
– [1]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|[2]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. CPT Pharmacometrics Syst Pharmacol. 2019 Jul;8(7):489-499.
CAS Number
– 2230757-47-6
Molecular Weight
– 481.51
Compound Purity
– 98.41
SMILES
– O=C(NC1=NC=CC=C1)C2=CC=C(C3=C4C(N)=NC=CN4C(C(CCCNC(C#CC)=O)=O)=N3)C=C2
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– DMSO : 250 mg/mL (ultrasonic)
Target
– Btk;Cytochrome P450;Drug Metabolite
Isoform
– CYP2;CYP3
Pathway
– Metabolic Enzyme/Protease;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
