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Quizartinib | Selective FLT3 Inhibitor

CAS:
950769-58-1

Catalog Number:
10-4813
Activity:
Selective FLT3 inhibitor
Chemical Name:
1-(5-(t-Butyl)isoxazol-3-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea
Alternate Names:
AC220
Molecular Weight:
560.67
Molecular Formula:
C29H32N6O4S
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Quizartinib (950769-58-1) is a potent and selective inhibitor of FLT3 (Kd = 1.6nM, IC50 = 0.56 nM MV4-11 cells).1 It is in clinical trials for treatment of Acute Myelogenous Leukemia (AML).2,3 Quizartinib priming resulted in prevention of myelosuppression in mice treated with 5-FU and Gemcitabine.4 Quizartinib showed significant reversal of ABCG2-mediated multidrug resistance (@ 3 µM) via antagonism of drug efflux function.5,6

References/Citations:

1) Chao et al. (2009) Identification of N-(5-tert-butyl-isoxazol-3-yl)-N’-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor; J. Med. Chem. 52 7808
2) Zarrinkar et al. (2009); AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia(AML); Blood 114 2984
3) Fathi and Chen (2017); The role of FLT3 inhibitors in the treatment of FLT3-mutated acute myeloid leukemia; Eur. J .Haematol. 98 330
4) Taylor and Langdon (2017); Hitting the snooze button: Inducing quiescence with the FLT3 inhibitor quizartinib protects hematopoietic progenitors from chemotherapy; Mol. Cell Oncol. 4 e1378156
5) Li et al. (2017); Quizartinib (AC220) reverses ABCG2-mediated multidrug resistance: In vitro and In vivo studies; Oncotarget 8 93785
6) Bhullar et al. (2013) The FLT3 inhibitor quizartinib inhibits ABCG2 at pharmacologically relevant concentrations, with implications for both chemosensitization and adverse drug reactions; PLoS One 8 e71266

Quizartinib | Selective FLT3 Inhibitor is also available in the Cellular Metabolism Library.

CAS:
950769-58-1

Catalog Number:
10-4813
Activity:
Selective FLT3 inhibitor
Chemical Name:
1-(5-(t-Butyl)isoxazol-3-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea
Alternate Names:
AC220
Molecular Weight:
560.67
Molecular Formula:
C29H32N6O4S
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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