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ACP-5862

CAT: 0804-HY-135334-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-135334-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
2230757-47-6
UNSPSC
12352005
Target
Btk; Cytochrome P450; Drug Metabolite
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/acp-5862.html
Concentration
10mM
Purity
98.32
Solubility
DMSO : 250 mg/mL (ultrasonic)
Smiles
O=C(NC1=NC=CC=C1)C2=CC=C(C3=C4C(N)=NC=CN4C(C(CCCNC(C#CC)=O)=O)=N3)C=C2
Molecular Formula
C26H23N7O3
Molecular Weight
481.51
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CYP2; CYP3

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