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Quizartinib

Inhibitor of FLT3 and ABC proteins
 
ENZ-CHM154-0001 1 mg 98.00 USD
 
ENZ-CHM154-0005 5 mg 169.00 USD
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Quizartinib (AC220) is a second-generation FLT3 inhibitor that has shown promising activity in Phase II clinical trials. It inhibits mutant and wild-type FLT3 in vivo at 0.1 and 0.5 µM, respectively, and has shown favorable activity and tolerability in phase I and II trials in acute myeloid leukemia, with QT prolongation as the dose-limiting toxicity. Recently, AC220 has also been shown to be an effective inhibitor of ATP-binding cassette (ABC) proteins ABCB1 (P-glycoprotein) and ABCG2 (breast cancer resistance protein). Quizartinib inhibited transport of fluorescent ABCG2 and ABCB1 substrates in ABCG2- and ABCB1-overexpressing cells in a concentration-dependent manner, from 0.1 to 5 µM and from 0.5 to 10 µM, respectively, and inhibited [125I]-IAAP photolabeling of ABCG2 and ABCB1 with IC50 values of 0.07 and 3.3 µM, respectively.

Product Details

Alternative Name:AC-220, 1-(5-tert-Butyl-1,2-oxazol-3-yl)-3-[4-[6-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl]urea
 
Formula:C29H32N6O4S
 
MW:560.7
 
CAS:950769-58-1
 
Purity:≥97% (HPLC)
 
Identity:Determined by EM-MS, NMR
 
Appearance:White powder.
 
Solubility:Soluble in DMSO (33mg/ml) or ethanol (0.5mg/ml).
 
Shipping:Ambient
 
Short Term Storage:+4°C
 
Long Term Storage:-20°C
 
Regulatory Status:RUO - Research Use Only
 
ENZ-CHM154 structure
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ENZ-CHM154 structure

Product Literature References

PARP1 PARylates and stabilizes STAT5 in FLT3-ITD acute myeloid leukemia and other STAT5-activated cancers: A.J. Dellomo, et al.; Transl. Oncol. 15, 101283 (2021), Abstract;

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