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 |
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| Formula: | C29H32N6O4S |
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| MW: | 560.7 |
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| CAS: | 950769-58-1 |
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| Purity: | ≥97% (HPLC) |
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| Identity: | Determined by EM-MS, NMR |
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| Appearance: | White powder. |
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| Solubility: | Soluble in DMSO (33mg/ml) or ethanol (0.5mg/ml). |
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| Shipping: | Ambient Temperature |
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| Short Term Storage: | +4°C |
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| Long Term Storage: | -20°C |
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| Regulatory Status: | RUO - Research Use Only |
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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;
