Quizartinib

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 50mg
ArtNr HY-13001-50mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
AC-220, AC220
CAS No.
950769-58-1
Purity
>98%
MW
5606672
Formula
C29H32N6O4S
Solubility
DMSO: >= 33 mg/mL
Biological Description
Quizartinib is a uniquely potent and selective Flt3 inhibitor with Kd (FLT3 binding affinity) of 1.6+/-0.7 nM in Biochemical assay.




IC50 & Target: Kd: 1.6+/-0.7 nM (Flt3)[1]
In Vitro: Quizartinib (AC220) is a novel compound expressly optimized as a FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). Quizartinib inhibits FLT3-WT and FLT3-ITD autophosphorylation with IC50 of 4.2+/-0.3 nM and 1.1+/-0.1 nM, respectively. Quizartinib inhibits MV4-11 and A375 cells with IC50 of 0.56+/-0.3 nM and >10 000 nM, respectively. Quizartinib inhibits FLT3 with low nanomolar potency in cellular assays and is highly selective when screened against the majority of the human protein kinome[1].
In Vivo: Quizartinib (AC220) inhibits FLT3 activity in vivo, significantly extends survival in a mouse model of FLT3-ITD AML at doses as low as 1 mg/kg when dosed orally once a day, eradicates tumors in a FLT3-dependent mouse xenograft model at 10 mg/kg, and potently inhibits FLT3 activity in primary patient cells. The oral bioavailability of Quizartinib, determined in rats by comparing oral and intravenous pharmacokinetics at 3 mg/kg, is approximately 40%. A single 10 mg/kg dose of Quizartinib is administered by oral gavage, and mice are killed at 2 time points after dosing, using groups of 4 animals each. Quantitation of total FLT3 and phospho-FLT3 in tumor samples revealed time-dependent inhibition of FLT3 autophosphorylation. FLT3 activity is inhibited by 90% at 2 hours, and 40% at 24 hours after administration. The extent of inhibition therefore correlated well with the expected free Quizartinib plasma levels, based on pharmacokinetic experiments[1].
Publications
Mol Cancer Ther. 2015 Oct; 14(10):2249-59.
Chem Biol. 2015 Aug 20; 22(8):1144-55.
Leukemia. 2012 Oct; 26(10):2233-44.
Cancer Cell. 2014 Feb 10; 25(2):226-42.
PLoS One. 2013; 8(2):e56473.
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 50mg
Lieferbar: In stock
Listenpreis: 190,36 €
Preis: 190,36 €
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