Quizartinib-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 Kd 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].

Product Specifications

CAS Number

[1300734-19-3]

Product Name Alternative

AC220-d8; AC708-d8

UNSPSC

12352005

Target

Apoptosis; FLT3; Isotope-Labeled Compounds; Ligands for Target Protein for PROTAC

Related Pathways

Apoptosis; Others; PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

[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

Molecular Formula

C29H24D8N6O4S

Molecular Weight

568.72

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[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.|[3]Sun X, et al. PROTACs: great opportunities for academia and industry. Signal Transduct Target Ther. 2019 Dec 24;4:64.|[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.