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ACP-5862-d4

CAT: 0804-HY-135334S-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-135334S-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-d4 is deuterium labeled ACP-5862. 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].
UNSPSC
12352005
Target
Btk; Cytochrome P450; Drug Metabolite; Isotope-Labeled Compounds
Type
Isotope-Labeled Compounds
Related Pathways
Metabolic Enzyme/Protease; Others; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Solubility
10 mM in DMSO
Smiles
O=C(NC1=NC([2H])=C([2H])C([2H])=C1[2H])C2=CC=C(C3=C4C(N)=NC=CN4C(C(CCCNC(C#CC)=O)=O)=N3)C=C2
Molecular Formula
C26H19D4N7O3
Molecular Weight
485.53
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[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.|[3]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
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

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