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Quizartinib dihydrochloride

Chemical Structure : Quizartinib dihydrochloride

CAS No.: 1132827-21-4

Quizartinib dihydrochloride (AC-220, AC220)

Catalog No.: PC-50013Not For Human Use, Lab Use Only.

Quizartinib dihydrochloride (AC220) is a potent, selective, second-generation FLT3 inhibitor with Kd of 1.6 nM, inhibits Wt FLT3 and FLT3-ITD autophosphorylation in MV4-11cell with IC50 of 4.2 and 1.1 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Quizartinib dihydrochloride (AC220) is a potent, selective, second-generation FLT3 inhibitor with Kd of 1.6 nM, inhibits Wt FLT3 and FLT3-ITD autophosphorylation in MV4-11cell with IC50 of 4.2 and 1.1 nM, respectively.
Quizartinib displays excellent kinase selectivity in a KinomeScan panel of 402 kinase binding assays, also potently inhibits PDGFRA, PDGFRB and RET.
Quizartinib inhibits MV4-11 cell proliferarion with IC50 of 0.56 nM, demonstrates antitumor efficacy in the MV4-11 tumor xenograft model.

Physicochemical Properties

M.Wt 633.589
Formula C29H34Cl2N6O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Zarrinkar PP, et al. Blood. 2009 Oct 1;114(14):2984-92.

2. Chao Q, et al. J Med Chem. 2009 Dec 10;52(23):7808-16.

3. Pratz KW, et al. Blood. 2010 Feb 18;115(7):1425-32.

4. Gunawardane RN, et al. Mol Cancer Ther. 2013 Apr;12(4):438-47.

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