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AC220

Chemical

C29H32N6O4S

560.7

950769-58-1

≥95%

Solid.

Soluble in DMSO. Slightly soluble (

Manufactured by SynKinase.

Target: PDGFR | Kinase Group: RTK | Substrate: TyrosineClick here for Original Manufacturer Product DatasheetOur product description may differ slightly from the original manufacturers product datasheet.

MKGMVQKQNTXMPT-UHFFFAOYSA-N

AMBIENT

+4°C

-20°C

Stable for at least 2 years after receipt when stored at -20°C.

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Quizartinib (AC220) is a second-generation FLT3 inhibitor that has shown promising activity in AML in Phase II clinical trials. It inhibits mutant and wild-type FLT3 in vivo at 0.1 and 0.5µM, 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 5µM and from 0.5 to 10µM, respectively, and inhibited [125I]-IAAP photolabeling of ABCG2 and ABCB1 with IC(50) values of 0.07 and 3.3µM, respectively.Product References

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML): P.P. Zarrinkar, et al.; Blood 114, 2984 (2009)

3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3): J.T. Hsu, et al.; Bioorg. Med. Chem. Lett. 22, 4654 (2012)