Anagrelide-¹³C₂,¹⁵N,d₂  (Synonyms: 阿那格雷-¹³C₂)

Anagrelide-¹³C₂,¹⁵N,d₂ is ¹⁵N and deuterated labeled Anagrelide (HY-B0523). Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC₅₀=36 nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action^[1][2][3].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
Anagrelide 有效抑制骨髓巨核细胞的发育 (IC₅₀=26?nM)^[2]。
Anagrelide (0.05、0.3、1 μM；12 天) 仅抑制巨核细胞生长，不抑制非巨核细胞生长^[3]。
Anagrelide (0.1-10000 nM) 在 GIST882 细胞系中诱导细胞毒性作用^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Anagrelide (5 mg/kg/bid；持续 10 天) 抑制或减少 GIST2B、GIST9、GIST882 模型中的肿瘤生长^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

262.11

C₉¹³C₂H₈D₂Cl₂N¹⁵NO

68475-42-3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Guosu Wang, et al. Comparison of the biological activities of Anagrelide and its major metabolites in haematopoietic cell cultures. Br J Pharmacol. 2005 Oct;146(3):324-32.  [Content Brief]

  [3]. Y Hong, et al. Comparison between Anagrelide and hydroxycarbamide in their activities against haematopoietic progenitor cell growth and differentiation: selectivity of Anagrelide for the megakaryocytic lineage. Leukemia. 2006 Jun;20(6):1117-22.  [Content Brief]

  [4]. Olli-Pekka Pulkka, et al. Anagrelide for Gastrointestinal Stromal Tumor. Clin Cancer Res. 2019 Mar 1;25(5):1676-1687.  [Content Brief]