Quizartinib (dihydrochloride)

Quizartinib dihydrochloride (AC220 dihydrochloride) is the dihydrochloride salt form of Quizartinib (HY-13001) . Quizartinib dihydrochloride is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib dihydrochloride inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib dihydrochloride can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib dihydrochloride induces apoptosis[1][2][3].

Product Specifications

CAS Number

[1132827-21-4]

Product Name Alternative

AC220 (dihydrochloride)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; FLT3; Ligands for Target Protein for PROTAC

Type

Reference compound

Related Pathways

Apoptosis; PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/quizartinib-dihydrochloride.html

Purity

99.81

Solubility

DMSO : 33.33 mg/mL (ultrasonic; adjust pH to 12 with 1 M NaOH)

Smiles

O=C(NC1=CC=C(C2=CN3C(SC4=CC(OCCN5CCOCC5)=CC=C34)=N2)C=C1)NC6=NOC(C(C)(C)C)=C6.[H]Cl.[H]Cl

Molecular Formula

C29H34Cl2N6O4S

Molecular Weight

633.59

Precautions

H302, H315, H319, H335

References & Citations

[1]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.|[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.