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Cat. No. M1641
AC220 Structure


Size Price Availability Quantity
10mM*1mL in DMSO USD 70  USD70 In stock
5mg USD 55  USD55 In stock
10mg USD 80  USD80 In stock
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Quality Control & Documentation
Biological Activity

AC220 (Quizartinib) is a orally-administered, potent and selective inhibitor of two receptor tyrosine kinases, FLT3 and KIT. AC220 is currently in a Phase 2 clinical study in the relapsed/refractory AML patient population with internal tandem duplication (ITD positive) activating mutations of the FLT3 kinase (FLT3-ITD positive). AC220 (Quizartinib) exhibits low nanomolar potency in biochemical and cellular assays and exceptional kinase selectivity, and in animal models is efficacious at doses as low as 1 mg/kg given orally once daily. While other agents showed some ability to clear leukemia from the circulating blood, AC220 has shown significant ability to clear leukemic cells from the bone marrow, where the disease originates. AC220-resistant FLT3 kinase domain mutants represent high-value targets for future FLT3 inhibitor development efforts.

Product Citations
Customer Product Validations & Biological Datas
Source Mol Cancer (2013). Figure 3. AC220
Method PCR
Cell Lines Ba/F3 cells
Concentrations 0 – 5000 nM
Incubation Time 48 h
Results Comparison of inhibition of cellular proliferation after quizartinib treatment revealed strong correlation between naturally occurring and engineered cell lines expressing identical mutant kinases
Source Mol Cancer (2013). Figure 2. AC220
Method cell apoptosis assay
Cell Lines leukemia cell line
Concentrations 0 – 5000 nM
Incubation Time 48 h
Results This finding suggests that the distinct mutant-KIT isoform directly orchestrates sensitivity towards quizartinib.
Protocol (for reference only)
Cell Experiment
Cell lines MV4-11 and RS4;11 cells
Preparation method Cellular assays. MV4-11 and RS4;11 cells were cultured in Iscove media with 10% fetal bovine serum (FBS) and RPMI complete with 10% FBS, respectively. For proliferation assays, cells were cultured overnight in low serum media (0.5% FBS), then seeded in a 96-well plate at 40 000 cells per well. Inhibitors were added to the cells and incubated at 37°C for 72 hours. Cell viability was measured using the Cell Titer-Blue Cell Viability Assay from Promega. To measure inhibition of FLT3 autophosphorylation, cells were cultured in low serum media (0.5% FBS) overnight and seeded at a density of 400 000 cells per well in a 96-well plate the following day. The cells were incubated with inhibitors for 2 hours at 37°C. To induce FLT3 autophosphorylation in RS4;11 cells, 100 ng/mL FLT3 ligand (R&D Systems) was added for 15 minutes after the 2-hour compound incubation. Cell lysates were prepared and incubated in 96-well plates precoated with a total FLT3 capture antibody (R&D Systems). The coated plates were incubated with either a biotinylated antibody against FLT3 (R&D Systems) to detect total FLT3 or an antibody against phosphotyrosines (Millipore) to detect FLT3 autophosphorylation. In both cases, a SULFO-tagged streptavidin secondary antibody was used for electrochemiluminescence detection on the Meso Scale Discovery platform.
Concentrations 0~10 µM
Incubation time 72 h
Animal Experiment
Animal models subcutaneous tumor model
Formulation 22% hydroxypropyl-β-cyclodextrin
Dosages 10 mg/kg
Administration orally
Chemical Information
Molecular Weight 560.67
Formula C29H32N6O4S
CAS Number 950769-58-1
Solubility (25°C) DMSO ≥100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Smith et al. Nature. Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia.

[2] Zarrinkar et al. Blood. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

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Keywords: AC220, Quizartinib supplier, FLT3, inhibitors, activators

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