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Purity: ≥98%
Quizartinib HCl (formerly AC220 and AC010220) is a novel, second-generation, and orally bioavailable FLT3 tyrosine kinase inhibitor for Flt3 (ITD/WT) with IC50 of 1.1 nM/4.2 nM in MV4-11 and RS4;11 cells, respectively, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Quizartinib has displayed potential anticancer activity. AC220 selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs), resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis. Mutations in FLT3, resulting in constitutive activation, are the most frequent genetic alterations in acute myeloid leukemia (AML) and occur in approximately one-third of AML cases. Quizartinib (Vanflyta) was approved in 2023 by FDA for treating AML.
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| References |
Blood.2009 Oct 1;114(14):2984-92.
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| Molecular Formula |
C29H34CL2N6O4S
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| Molecular Weight |
633.59
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| CAS # |
1132827-21-4
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| Related CAS # |
1132827-21-4 (HCl);950769-58-1;
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| SMILES |
O=C(NC1=CC=C(C(N=C2SC3=C4)=CN2C3=CC=C4OCCN5CCOCC5)C=C1)NC6=NOC(C(C)(C)C)=C6
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| InChi Key |
CVWXJKQAOSCOAB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H32N6O4S/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22-18-35-23-9-8-21(16-24(23)40-28(35)31-22)38-15-12-34-10-13-37-14-11-34/h4-9,16-18H,10-15H2,1-3H3,(H2,30,32,33,36)
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| Chemical Name |
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
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| Synonyms |
AC220 HCl or AC010220 HCl; AC220 diHCl; AC 220; AC-220 dihydrochloride; AC010220; AC-010220; AC 010220; AC010220
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5783 mL | 7.8915 mL | 15.7831 mL | |
| 5 mM | 0.3157 mL | 1.5783 mL | 3.1566 mL | |
| 10 mM | 0.1578 mL | 0.7892 mL | 1.5783 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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