「同位素标记抑制剂」ACP-5862-d4
【产品介绍】:
生物活性: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].
体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.
ACP-5862-d4 相关抗体:
Cytochrome C Antibody
Cytochrome P450 17A1 Antibody
Phospho-BTK(Y223) Antibody
Aromatase Antibody
BTK Antibody (YA816)
CYP11A1 Antibody
Cytochrome P450 1B1 Antibody (YA1836)
FMO3 Antibody (YA1992)
Adrenodoxin Antibody (YA2005)
Cytochrome P450 27A1 Antibody (YA2163)
Cytochrome P450 2C9 Antibody (YA2166)
Cytochrome P450 2E1 Antibody (YA2302)
Cytochrome P450 Reductase Antibody (YA2619)
Thromboxane A Synthase Antibody (YA2670)
Cytochrome P450 3A4 Antibody (YA3365)
HSD11B1 Antibody (YA3376)
Cytochrome P450 17A1 Antibody (YA786)
CYP2E1 Antibody
CYP1A2 Antibody
PLSCR3 Antibody (YA1672)
PROX1 Antibody (YA1754)
Cytochrome P450 4A Antibody (YA2087)
Cytochrome P450 24A1 Antibody (YA2121)
Tec Antibody (YA2181)
Cytochrome P450 26A1 Antibody (YA2259)
COX5B Antibody (YA2550)
Steroidogenic Factor 1 Antibody (YA3166)
Dynein Light Chain Tctex Type 1 Antibody (YA3263)
Cytochrome P450 2D6 Antibody (YA3384)
分子量:485.53
Formula:C26H19D4N7O3
非标记 CAS:2230757-47-6
运输条件:Room temperature in continental US; may vary elsewhere.
储存方式:Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (531 KB)
产品使用指南 (1538 KB)
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
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[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
[Content Brief]
[3]. 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.
[Content Brief]