Quizartinib (AC220)

For research use only.

Catalog No.S1526

68 publications

Quizartinib (AC220) Chemical Structure

CAS No. 950769-58-1

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. Quizartinib (AC220) induces apoptosis of tumor cells. Phase 3.

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Selleck's Quizartinib (AC220) has been cited by 68 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. Quizartinib (AC220) induces apoptosis of tumor cells. 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 M1HQNWZ2dmO2aX;uJGF{e2G7 M2\iflAvOS1zMDFOwG0> NELXU|E{OCCvaX6= MlHT[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NVz0[lljOjN7NkexO|c>
K562/ABCB1 NHn1PGhHfW6ldHnvckBCe3OjeR?= NHHuOoExNjFvMUCg{txO NEnte4M{OCCvaX6= M{fxUYVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MlywNlM6PjdzN{e=
8226/MR20  M3zHV2Z2dmO2aX;uJGF{e2G7 M2rhO|AvOS1zMDFOwG0> NFLKbXA{OCCvaX6= MXnlcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NV3sbG9COjN7NkexO|c>
K562/ABCG2 M17IcWZ2dmO2aX;uJGF{e2G7 NX61WWhVOC5zLUGwJO69VQ>? Mn;kN|AhdWmw Mlq3[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MojvNlM6PjdzN{e=
MCF-7 FLV1000 NUTObWQ6U2mwYYPlJGF{e2G7 MXew5qCUOzBiwsXN MWi1JI1qdg>? MnL6[IVkemWjc3XzJHsyOjWLXT3JRWFRKHCqb4TvcIFj\Wyrbnegc4YhSUKFQkGgZZQhUUN3MDDv[kA{NjNizszN NFzXN2IzOzl4N{G3Oy=>
MCF-7 FLV1000 NVLBXmVQU2mwYYPlJGF{e2G7 MXGw5qCUOzBiwsXN M3vlWFUhdWmw MVrk[YNz\WG|ZYOgX|EzPUmfLVnBRXAheGixdH;sZYJmdGmwZzDv[kBCSkOEMjDheEBKSzVyIH;mJFAvODdizszN NH7yTXAzOzl4N{G3Oy=>
K562/ABCG2 NXXJZmh[S2WubDDWbYFjcWyrdImgRZN{[Xm| NILDPW8xNjFxMD61M|EhyrWP MXS5OkBp M1L6TJNmdnOrdHn6[ZMhUzV4Mj;BRmNIOiClZXzsd{B1dyCvaYTvfIFvfHKxbnWgeI9xd3SnY3HuxsA> M4fzW|I{QTZ5MUe3
8226/MR20 NEnx[29E\WyuIG\pZYJqdGm2eTDBd5NigXN? Ml65NE4yKML3TR?= M3TSOlk3KGh? M4HNUpNmdnOrdHn6[ZMhUzV4Mj;BRmNIOiClZXzsd{B1dyCvaYTvfIFvfHKxbnWgeI9xd3SnY3HuxsA> NWDXZmdLOjN7NkexO|c>
HMC1.1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTBWG5qUUN3ME2xOEBvVQ>? MVGyN|Q6PzNzNx?=
HMC1.2 M3\lTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTVTWM2OD1zN{K3JI5O NXSyVHptOjN2OUezNVc>
p815 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoX6TWM2OD12NEWgcm0> MXGyN|Q6PzNzNx?=
Kasumi-1 MkLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPkcVhKSzVyPUO2JI5O MXiyN|Q6PzNzNx?=
M-07e + SCF Mm\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rKOWlEPTB;N{egcm0> NVzDUWlIOjN2OUezNVc>
EOL-1 NIHOPY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHiTWM2OD1zIH7N MlnJNlM1QTd|MUe=
MV4;11 Mlf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\qTWM2ODxiMTDuUS=> MmHnNlM1QTd|MUe=
MOLM14 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRCBzIH7N MV6yN|Q6PzNzNx?=
Pat.221 MoHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHUUlFKSzVyPU[3OUBvVQ>? M1HUUlI{PDl5M{G3
Pat.279 NHXXU4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTN2M{Sgcm0> M1HIUlI{PDl5M{G3
Pat.299 M1TxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHpNlViUUN3ME23NlQ5KG6P NX\EXYE4OjN2OUezNVc>
Pat.305 NW\HPI5oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofxTWM2OD15MEe5JI5O NYntSWJROjN2OUezNVc>
Pat.375 NWHsUG45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3IZ5BKSzVyPUWwN{BvVQ>? NWXXOJozOjN2OUezNVc>
Pat.379 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPIUnQ2UUN3ME24NFYhdk1? MWGyN|Q6PzNzNx?=
Pat.368 M1LtNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTJ5MECgcm0> MVOyN|Q6PzNzNx?=
Pat.601 MojyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmOzTWM2OD1zMUWzJI5O M2\pflI{PDl5M{G3
HMC1.1 NH2zSnNCeG:ydH;zbZMhSXO|YYm= MmDzTWM2OD1|MTDuUS=> M2D2cFI{PDl5M{G3
p815 NYnnO4l7SXCxcITvd4l{KEG|c3H5 NWnCbpdOUUN3ME2zOFEhdk1? MoHrNlM1QTd|MUe=
Kasumi-1 NUXyR2w3SXCxcITvd4l{KEG|c3H5 NWPidYtCUUN3ME22O{BvVQ>? NFvUfXIzOzR7N{OxOy=>
M-07e + SCF NXvGOol6SXCxcITvd4l{KEG|c3H5 NXzIeXZIUUN3ME23PEBvVQ>? NFLVbmozOzR7N{OxOy=>
EOL-1 MXPBdI9xfG:|aYOgRZN{[Xl? NGDVWmRKSzVyPDCxJI5O NU\vbWRwOjN2OUezNVc>
MV4;11 MkDzRZBweHSxc3nzJGF{e2G7 MUnJR|UxRTJibl2= NYTySnczOjN2OUezNVc>
MOLM14 MljiRZBweHSxc3nzJGF{e2G7 Mkj5TWM2OD1|IH7N NU\FOGFiOjN2OUezNVc>
GIST822 M4\hV2Fxd3C2b4Ppd{BCe3OjeR?= M3vSR2lEPTB;MUC5JI5O NIHuV5kzOzR7N{OxOy=>
Pat.368 M2Hq[GFxd3C2b4Ppd{BCe3OjeR?= M3HYfGlEPTB;Mkm5PEBvVQ>? NFn0ZXMzOzR7N{OxOy=>
Pat.601 NEOwN29CeG:ydH;zbZMhSXO|YYm= NY\JTYpMUUN3ME24O|Yhdk1? MnfCNlM1QTd|MUe=
MV4-11 NVTheJJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXnSld5PzJiaB?= M1qydWlEPTB;MD6zJI5O NIqxTlAzOzRzMkmzNS=>
MOLM-14 M{fNbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlGyO|IhcA>? NEOwbHFKSzVyPUCuNUBvVQ>? MlvBNlM1OTJ7M{G=
SEM-K2 NU\SUFdpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvEN2o4OiCq MU\JR|UxRTBwNDDuUS=> NFrZVHMzOzRzMkmzNS=>
RS4;11 MnTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn6NXk4OiCq M1LwSmlEPTB-MUCsNFAxKG6P MoHCNlM1OTJ7M{G=
THP-1 NXP2NFhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWe3NkBp M1XBbmlEPTB-MUCsNFAxKG6P NXzlWYhoOjN2MUK5N|E>
MV4-11 NXXCPXZuSXCxcITvd4l{KEG|c3H5 Ml;IPE8zPCCq NF\aWpJqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? M2[xOlI{PDF{OUOx
MOLM-14 M{\HTGFxd3C2b4Ppd{BCe3OjeR?= MVu4M|I1KGh? MYrpcoR2[2W|IIPp[45q\mmlYX70JIFv\CCmb4PlMYRmeGWwZHXueEBRSVKSIHPs[YF3[WenIHHu[EBi[2O3bYXsZZRqd25ib3[gd5VjNTKQIFTORS=> NXLFOXZXOjN2MUK5N|E>
SEM-K2 MXjBdI9xfG:|aYOgRZN{[Xl? MV:4M|I1KGh? MWfpcoR2[2W|IIPp[45q\mmlYX70JIFv\CCmb4PlMYRmeGWwZHXueEBRSVKSIHPs[YF3[WenIHHu[EBi[2O3bYXsZZRqd25ib3[gd5VjNTKQIFTORS=> M2HXfVI{PDF{OUOx
MV4-11 NV74W|hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGn5[I44OiCq Mk\nTWM2OD1yLkW2JOKyKDBwMzDuUS=> NISyfJYyQTZ3NESwPC=>
A375 M4jLTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13KNlczKGh? M{nHeWlEPTB-IEGwJFAxOCCwTR?= MoTNNVk3PTR2MEi=

... 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]
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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]
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  • 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=CN4C5=C(C=C(C=C5)OCCN6CCOCC6)SC4=N3

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04459585 Recruiting Drug: Dabigatran Etexilate Mesylate|Drug: Quizartinib Healthy Subjects|Drug-drug Interaction|Pharmacokinetics|Quizartinib Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. September 16 2020 Early Phase 1
NCT04459598 Recruiting Drug: Efavirenz|Drug: Quizartinib Healthy Subjects|Drug-drug Interaction|Pharmacokinetics|Quizartinib Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. September 9 2020 Early Phase 1
NCT04473664 Not yet recruiting Drug: Quizartinib Hepatic Impairment|Moderate Impaired Hepatic Function Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. September 23 2020 Phase 1
NCT04209725 Recruiting Drug: CPX-351|Drug: Quizartinib Leukemia Myeloid Acute SCRI Development Innovations LLC June 3 2020 Phase 2
NCT02984995 Completed Drug: Quizartinib Leukemia Myeloid Acute Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. December 8 2016 Phase 2

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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