Quizartinib-d₈  (Synonyms: AC220-d₈; AC708-d₈)

Quizartinib-d₈ (AC220-d₈) is deuterium labeled Quizartinib. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a K_d of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC₅₀s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis^[1].

氢、碳和其他元素的稳定重同位素已被掺入药物分子中，主要用作药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注。

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

568.72

AC220-d₈; AC708-d₈

C₂₉H₂₄D₈N₆O₄S

1300734-19-3

950769-58-1

奎扎替尼-d₈

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;53(2):211-216.  [Content Brief]

  [2]. Puissant A, et al. SYK is a critical regulator of FLT3 in acute myeloid leukemia. Cancer Cell. 2014 Feb 10;25(2):226-42.  [Content Brief]

  [3]. Sun X, et al. PROTACs: great opportunities for academia and industry. Signal Transduct Target Ther. 2019 Dec 24;4:64.  [Content Brief]

  [4]. Zarrinkar PP, et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood, 2009, 114(14), 2984-2992.  [Content Brief]