Quizartinib (AC220)

For research use only.

Catalog No.S1526

63 publications

Quizartinib (AC220) Chemical Structure

Molecular Weight(MW): 560.67

Quizartinib (AC220) is a second-generation FLT3 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. Phase 3.

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Selleck's Quizartinib (AC220) has been cited by 63 publications

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Biological Activity

Description Quizartinib (AC220) is a second-generation FLT3 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. Phase 3.
Features The most potent cellular FLT3-ITD inhibitor.
Targets
FLT3 (ITD) [1]
(MV4-11 cells)
FLT3 (WT) [1]
(RS4;11 cells)
1.1 nM 4.2 nM
In vitro

AC220, a unique, potent and selective inhibitor of FLT3, has high affinity for FLT3 with a Kd value of 1.6 nM. AC220 inhibits the autophosphorylation of FLT3 in the human leukemia cell lines MV4-11 which harbor a homozygous FLT3-ITD mutation and is FLT3 dependent, and RS4;11 which expresses wild-type FLT3 with IC50 values of 1.1 nM and 4.2 nM, respectively. AC220 is the most potent cellular FLT3-ITD inhibitor, leading to the most significant inhibition of MV4-11 cell proliferation with IC50 of 0.56 nM compared to all other FLT3 inhibitors whose IC50 values range from 0.87 nM to 64 nM. AC220 has no inhibitory activity against the proliferation of A375 cells which harbor an activating mutation in BRAF and are not FLT3 dependent, indicating a large window between FLT3 inhibition and general cytotoxic effects. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60/VCR M{[xdmZ2dmO2aX;uJGF{e2G7 NUP2T2JDOC5zLUGwJO69VQ>? NVv0PFVtOzBibXnu MXrlcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MWSyN|k3PzF5Nx?=
K562/ABCB1 MUfGeY5kfGmxbjDBd5NigQ>? M2\BeVAvOS1zMDFOwG0> MYSzNEBucW5? NUXseIl3\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MmO3NlM6PjdzN{e=
8226/MR20  NHG2TWVHfW6ldHnvckBCe3OjeR?= M2P1SlAvOS1zMDFOwG0> M1nPXVMxKG2rbh?= MlLo[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NIDyVW0zOzl4N{G3Oy=>
K562/ABCG2 NFL0enRHfW6ldHnvckBCe3OjeR?= MmS1NE4yNTFyIN88US=> MYezNEBucW5? MYXlcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MVmyN|k3PzF5Nx?=
MCF-7 FLV1000 MXPLbY5ie2ViQYPzZZk> M4LGe|DjiJN|MDFCuW0> M2jsR|UhdWmw NYXYVGUz\GWlcnXhd4V{KFtzMkXJYU1KSUGSIIDoc5RwdGGkZXzpcochd2ZiQVLDRlEh[XRiSVO1NEBw\iB|LkOg{txO Mn\ENlM6PjdzN{e=
MCF-7 FLV1000 MmPpT4lv[XOnIFHzd4F6 NYfpTIJkOOLCk{OwJOK2VQ>? NEjsN3E2KG2rbh?= MWLk[YNz\WG|ZYOgX|EzPUmfLVnBRXAheGixdH;sZYJmdGmwZzDv[kBCSkOEMjDheEBKSzVyIH;mJFAvODdizszN NXvuZWZuOjN7NkexO|c>
K562/ABCG2 M3PhZWNmdGxiVnnhZoltcXS7IFHzd4F6ew>? MV2wMlEwOC53L{GgxtVO NF75[WU6PiCq M3LCV5NmdnOrdHn6[ZMhUzV4Mj;BRmNIOiClZXzsd{B1dyCvaYTvfIFvfHKxbnWgeI9xd3SnY3HuxsA> NVTpWVdMOjN7NkexO|c>
8226/MR20 MmnCR4VtdCCYaXHibYxqfHliQYPzZZl{ NVrVO4U5OC5zINM1US=> NXjvfmNtQTZiaB?= NHf5[G9{\W6|aYTpfoV{KEt3NkKvRWJETzJiY3XscJMhfG9ibXn0c5hidnS{b37lJJRweG:2ZXPhcuKh M3vjXlI{QTZ5MUe3
HMC1.1 Moj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorCTWM2OD1zNDDuUS=> M3naU|I{PDl5M{G3
HMC1.2 NUnENodXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF65[lRKSzVyPUG3Nlchdk1? M{e0d|I{PDl5M{G3
p815 M1W2b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3ETWM2OD12NEWgcm0> M2fhRlI{PDl5M{G3
Kasumi-1 NVLnVZFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTN4IH7N Mn3NNlM1QTd|MUe=
M-07e + SCF M1zQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XkSWlEPTB;N{egcm0> NHzLT3gzOzR7N{OxOy=>
EOL-1 MlziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTFibl2= NXTSemk2OjN2OUezNVc>
MV4;11 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nieWlEPTB:IEGgcm0> MkPUNlM1QTd|MUe=
MOLM14 NULUepp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRCBzIH7N MoXCNlM1QTd|MUe=
Pat.221 MofIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTZ5NTDuUS=> MYWyN|Q6PzNzNx?=
Pat.279 NXy2TXRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PLVWlEPTB;M{SzOEBvVQ>? MoPpNlM1QTd|MUe=
Pat.299 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoC3TWM2OD15MkS4JI5O M2mySVI{PDl5M{G3
Pat.305 NIWxR5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlToTWM2OD15MEe5JI5O NUXLUWlTOjN2OUezNVc>
Pat.375 M3\aVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2S5UWlEPTB;NUCzJI5O MWeyN|Q6PzNzNx?=
Pat.379 NXrBOlJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\LfGlEPTB;OEC2JI5O MYGyN|Q6PzNzNx?=
Pat.368 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17MeWlEPTB;MkewNEBvVQ>? M4qxe|I{PDl5M{G3
Pat.601 M{Lyd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\HWWlEPTB;MUG1N{BvVQ>? MkX2NlM1QTd|MUe=
HMC1.1 Mnj6RZBweHSxc3nzJGF{e2G7 NGLhW5JKSzVyPUOxJI5O NXezW|k3OjN2OUezNVc>
p815 MUHBdI9xfG:|aYOgRZN{[Xl? NGLNOJNKSzVyPUO0NUBvVQ>? NIPm[oEzOzR7N{OxOy=>
Kasumi-1 Mnv4RZBweHSxc3nzJGF{e2G7 NHjqTHVKSzVyPU[3JI5O MVGyN|Q6PzNzNx?=
M-07e + SCF M3G4OGFxd3C2b4Ppd{BCe3OjeR?= M{W2e2lEPTB;N{igcm0> M2rMUlI{PDl5M{G3
EOL-1 MlrURZBweHSxc3nzJGF{e2G7 M{Hab2lEPTB:IEGgcm0> NInNV4szOzR7N{OxOy=>
MV4;11 NHLnVG1CeG:ydH;zbZMhSXO|YYm= NEDu[FhKSzVyPUKgcm0> MVeyN|Q6PzNzNx?=
MOLM14 M3XhVmFxd3C2b4Ppd{BCe3OjeR?= NUjJ[IQ2UUN3ME2zJI5O MmfGNlM1QTd|MUe=
GIST822 NGjnOZZCeG:ydH;zbZMhSXO|YYm= M2n3dGlEPTB;MUC5JI5O MWOyN|Q6PzNzNx?=
Pat.368 MnzERZBweHSxc3nzJGF{e2G7 NGCzZVJKSzVyPUK5PVghdk1? MX[yN|Q6PzNzNx?=
Pat.601 NV\KUGlvSXCxcITvd4l{KEG|c3H5 MYjJR|UxRTh5NjDuUS=> NH\DXlEzOzR7N{OxOy=>
MV4-11 NWqwRmtYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7NTYc4OiCq MnjxTWM2OD1yLkOgcm0> NEPWV3YzOzRzMkmzNS=>
MOLM-14 NFTPb3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{WyTlczKGh? NXzhTlk6UUN3ME2wMlEhdk1? M1LLNlI{PDF{OUOx
SEM-K2 MmPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml60O|IhcA>? NVnRN4dnUUN3ME2wMlQhdk1? NX7jPYN7OjN2MUK5N|E>
RS4;11 NHX2PJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3P5PFczKGh? NV\ZSnRDUUN3ME6xNEwxODBibl2= NV7LTlc4OjN2MUK5N|E>
THP-1 NImwNYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zWelczKGh? Mkm1TWM2OD5zMDywNFAhdk1? MWGyN|QyOjl|MR?=
MV4-11 NXnIblVESXCxcITvd4l{KEG|c3H5 MlnCPE8zPCCq NF;ONJdqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? MXmyN|QyOjl|MR?=
MOLM-14 MVfBdI9xfG:|aYOgRZN{[Xl? M3rLR|gwOjRiaB?= NGr4fW5qdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? NYjXWo9HOjN2MUK5N|E>
SEM-K2 NWXPVYhKSXCxcITvd4l{KEG|c3H5 NVHv[oxzQC9{NDDo NYTlfHdrcW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? NFnj[FgzOzRzMkmzNS=>
MV4-11 MmHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jEXFczKGh? MYTJR|UxRTBwNU[gxtEhOC5|IH7N MlXENVk3PTR2MEi=
A375 NHjEUXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7ESmM4OiCq MkPRTWM2OD5iMUCgNFAxKG6P MonVNVk3PTR2MEi=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT5 / STAT5 / β-catenin / p-AKT / AKT / p-ERK / ERK / p-S6 / S6; 

PubMed: 28625976     


Western blot analysis of AC220 treated MV4-11 cells. Cells were starved for overnight and treated with AC220 at indicated concentrations. Cells were harvested after 2 hours treatment and lysed. Then western blots analysis was performed. The quantification of bands are shown below the gel.

phospho-FLT3 / FLT3; 

PubMed: 22875611     


(B) The same cells were also harvested for Western blot analysis after treatment for 90 min with different concentrations of AC220. The phosphorylation of the different FLT3 proteins was determined using a phospho-FLT3 antibody.

28625976 22875611
Immunofluorescence
WGA / FLT3 ; 

PubMed: 28895560     


Immunofluorescence staining of FLT3-WT, FLT3 mutants or empty vector with or without AC220 treatment in transiently transfected U2OS cells. WGA (wheat germ agglutinin). Scale bar: 25 μm.

28895560
Growth inhibition assay
Cell viability; 

PubMed: 23967177     


K562/ABCB1 and K562/ABCG2 cells exhibit collateral sensitivity toquizartinib. K562, K562/ABCB1 and K562/ABCG2 cells were plated in the presence of quizartinib in increasing concentrations for 96 hours and viable cells were measured using the WST-1 assay.

23967177
In vivo Oral administration of AC220 (10 mg/kg) induces time-dependent inhibition of FLT3 autophosphorylation in the FLT3-ITD–dependent MV4-11 tumor xenograft mouse model; the inhibition being 90% at 2 hours and 40% at 24 hours. AC220 significantly extends survival in a mouse model of FLT3-ITD AML with doses as low as 1 mg/kg given orally once a day. Treatment with AC220 at 10 mg/kg for 28 days results in rapid and complete regression of tumors in all mice with no tumor regrowth during the 60-day posttreatment period. AC220 displays more significant efficacy compared to sunitinib treatment which causes tumors to shrink slowly and resume growth immediately upon discontinuation of treatment in all but one of the mice. [1]

Protocol

Kinase Assay:[1]
- Collapse

Inhibition of FLT3 autophosphorylation:

To measure inhibition of FLT3 autophosphorylation, MV4-11 or RS4;11 cells are 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 are incubated with different concentrations of AC220 for 2 hours at 37 °C. To induce FLT3 autophosphorylation in RS4;11 cells, 100 ng/mL FLT3 ligand is added for 15 minutes after the 2-hour AC220 incubation. Cell lysates are prepared and incubated in 96-well plates precoated with a total FLT3 capture antibody. The coated plates are incubated with either a biotinylated antibody against FLT3 to detect total FLT3 or an antibody against phosphotyrosines to detect FLT3 autophosphorylation. In both cases, a SULFO-tagged streptavidin secondary antibody is used for electrochemiluminescence detection on the Meso Scale Discovery platform. The concentration of AC220 that inhibits FLT3-ITD or TLT3-WT autophosphorylation by 50% represents IC50 value
Cell Research:[1]
- Collapse
  • Cell lines: MV4-11 and RS4;11 cells
  • Concentrations: Dissolved in DMSO, final concentration ~20 μM
  • Incubation Time: 72 hours
  • Method: Cells are cultured overnight in low serum media (0.5% FBS), seeded in a 96-well plate at 40 000 cells per well and exposed to AC220 for 72 hours at 37 °C. Cell viability is measured using the Cell Titer-Blue Cell Viability Assa
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Female NU/NU or severe combined immunodeficient mice implanted with MV4-11 cells
  • Dosages: ~10 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 33 mg/mL (58.85 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
15% Captisol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 560.67
Formula

C29H32N6O4S

CAS No. 950769-58-1
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)(C)C1=CC(=NO1)NC(=O)NC2=CC=C(C=C2)C3=C[N]4C(=N3)SC5=CC(=CC=C45)OCCN6CCOCC6

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04209725 Not yet recruiting Drug: CPX-351|Drug: Quizartinib Leukemia Myeloid Acute SCRI Development Innovations LLC March 2020 Phase 2
NCT02984995 Completed Drug: Quizartinib Leukemia Myeloid Acute Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. December 8 2016 Phase 2
NCT02668653 Active not recruiting Drug: Chemotherapy|Drug: Quizartinib|Drug: Placebo Acute Myeloid Leukemia|Leukemia Daiichi Sankyo Inc. September 2016 Phase 3
NCT02675478 Completed Drug: AC220 Relapsed AML|Refractory AML Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. February 2016 Phase 1

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Frequently Asked Questions

  • Question 1:

    Is it possible to alter the captisol concentration to make it more dissolvable i.e 20% or 25% captisol ?

  • Answer:

    In 15% Captisol, the compound forms s suspension at 30mg/ml. Increasing the percentage of Captisol will not convert the mixture into solution. You can use suspension for oral gavage feeding.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID