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].

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.

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

568.72

C₂₉H₂₄D₈N₆O₄S

1300734-19-3

950769-58-1

[2H]C1([2H])C([2H])([2H])OC([2H])([2H])C([2H])([2H])N1CCOC2=CC=C(N3C(S4)=NC(C5=CC=C(C=C5)NC(NC6=NOC(C(C)(C)C)=C6)=O)=C3)C4=C2

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]