Quizartinib (AC220)

Catalog No.S1526

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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Cited by 26 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 NEnVcGFHfW6ldHnvckBCe3OjeR?= MoW2NE4yNTFyIN88US=> NWTKbmlXOzBibXnu NGW1TYRmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MXOyN|k3PzF5Nx?=
K562/ABCB1 M3\GU2Z2dmO2aX;uJGF{e2G7 M2DrSlAvOS1zMDFOwG0> MoD5N|AhdWmw M1GwR4VvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MnftNlM6PjdzN{e=
8226/MR20  MXPGeY5kfGmxbjDBd5NigQ>? M2n5SlAvOS1zMDFOwG0> MWezNEBucW5? MmXR[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NVzOd|dlOjN7NkexO|c>
K562/ABCG2 NFfoXlFHfW6ldHnvckBCe3OjeR?= NGW4SIkxNjFvMUCg{txO NWPT[WQxOzBibXnu M{DlZYVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NITDcJczOzl4N{G3Oy=>
MCF-7 FLV1000 MYfLbY5ie2ViQYPzZZk> MYmw5qCUOzBiwsXN NIX5dlY2KG2rbh?= NWXPVZN6\GWlcnXhd4V{KFtzMkXJYU1KSUGSIIDoc5RwdGGkZXzpcochd2ZiQVLDRlEh[XRiSVO1NEBw\iB|LkOg{txO MoToNlM6PjdzN{e=
MCF-7 FLV1000 M2Hrb2tqdmG|ZTDBd5NigQ>? MVmw5qCUOzBiwsXN NFj3fYE2KG2rbh?= MlXq[IVkemWjc3XzJHsyOjWLXT3JRWFRKHCqb4TvcIFj\Wyrbnegc4YhSUKFQkKgZZQhUUN3MDDv[kAxNjB5IN88US=> NUfCdXNTOjN7NkexO|c>
K562/ABCG2 MUXD[YxtKF[rYXLpcIl1gSCDc4PhfZM> Ml3PNE4yNzBwNT:xJOK2VQ>? NXjoXY9qQTZiaB?= NWrGXIpme2Wwc3n0bZpmeyCNNU[yM2FDS0d{IHPlcIx{KHSxIH3peI95[W62cn;u[UB1d3CxdHXjZY7DqA>? M4TveFI{QTZ5MUe3
8226/MR20 NHzCXYdE\WyuIG\pZYJqdGm2eTDBd5NigXN? Ml65NE4yKML3TR?= M1zvelk3KGh? M1zqNJNmdnOrdHn6[ZMhUzV4Mj;BRmNIOiClZXzsd{B1dyCvaYTvfIFvfHKxbnWgeI9xd3SnY3HuxsA> MoTCNlM6PjdzN{e=
HMC1.1 MlTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLXVYxPUUN3ME2xOEBvVQ>? NEHBOW0zOzR7N{OxOy=>
HMC1.2 NWD6UYFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1u3U2lEPTB;MUeyO{BvVQ>? NGPwPHMzOzR7N{OxOy=>
p815 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVq0ZndxUUN3ME20OFUhdk1? MXmyN|Q6PzNzNx?=
Kasumi-1 NW\6eWtrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnJVItKSzVyPUO2JI5O MmC0NlM1QTd|MUe=
M-07e + SCF MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LpemlEPTB;N{egcm0> MVSyN|Q6PzNzNx?=
EOL-1 NH:wd|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fXNmlEPTB;MTDuUS=> NWroUmN1OjN2OUezNVc>
MV4;11 M{XjTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fsTWlEPTB:IEGgcm0> NFXqOXEzOzR7N{OxOy=>
MOLM14 MkDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3lUGxKSzVyPDCxJI5O NU\1N5NvOjN2OUezNVc>
Pat.221 NFTt[2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTZ5NTDuUS=> NYHIOlhtOjN2OUezNVc>
Pat.279 NG\R[2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnDWXYzUUN3ME2zOFM1KG6P NVTFfZhUOjN2OUezNVc>
Pat.299 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTd{NEigcm0> M3HG[lI{PDl5M{G3
Pat.305 NHnOdIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7Pd5NKSzVyPUewO|khdk1? MVqyN|Q6PzNzNx?=
Pat.375 Ml3IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVSwTlNEUUN3ME21NFMhdk1? MnmwNlM1QTd|MUe=
Pat.379 NHvSNnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfKNI16UUN3ME24NFYhdk1? Ml3NNlM1QTd|MUe=
Pat.368 NXrhOZhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmG3TWM2OD1{N{CwJI5O NV71SXNmOjN2OUezNVc>
Pat.601 M1jZPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\mTWM2OD1zMUWzJI5O M1i1WlI{PDl5M{G3
HMC1.1 M4C5[WFxd3C2b4Ppd{BCe3OjeR?= NHjmOGxKSzVyPUOxJI5O MlfINlM1QTd|MUe=
p815 M4\3UmFxd3C2b4Ppd{BCe3OjeR?= Mo\3TWM2OD1|NEGgcm0> MoK1NlM1QTd|MUe=
Kasumi-1 MYrBdI9xfG:|aYOgRZN{[Xl? MU\JR|UxRTZ5IH7N M4LDVFI{PDl5M{G3
M-07e + SCF MULBdI9xfG:|aYOgRZN{[Xl? MVrJR|UxRTd6IH7N MnrRNlM1QTd|MUe=
EOL-1 MmPlRZBweHSxc3nzJGF{e2G7 MUDJR|UxRCBzIH7N MWiyN|Q6PzNzNx?=
MV4;11 NX:xZ3h{SXCxcITvd4l{KEG|c3H5 M2\rUWlEPTB;MjDuUS=> M{PDPVI{PDl5M{G3
MOLM14 MYjBdI9xfG:|aYOgRZN{[Xl? MkP6TWM2OD1|IH7N NH\tOGczOzR7N{OxOy=>
GIST822 MXjBdI9xfG:|aYOgRZN{[Xl? NWTmVpdKUUN3ME2xNFkhdk1? Mni5NlM1QTd|MUe=
Pat.368 NHTFVlVCeG:ydH;zbZMhSXO|YYm= NXXUUlE2UUN3ME2yPVk5KG6P NGfsdJkzOzR7N{OxOy=>
Pat.601 NFPtWGJCeG:ydH;zbZMhSXO|YYm= MUjJR|UxRTh5NjDuUS=> MXeyN|Q6PzNzNx?=
MV4-11 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkezO|IhcA>? Mom4TWM2OD1yLkOgcm0> MYSyN|QyOjl|MR?=
MOLM-14 NIHXS2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\lO|IhcA>? M1HWZWlEPTB;MD6xJI5O NWDkemFnOjN2MUK5N|E>
SEM-K2 NUPTcVRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUG3NkBp NVPpV3duUUN3ME2wMlQhdk1? NFLJU3MzOzRzMkmzNS=>
RS4;11 MlS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV63NkBp Mmq2TWM2OD5zMDywNFAhdk1? M1u4RlI{PDF{OUOx
THP-1 M3XLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO3NkBp MnL1TWM2OD5zMDywNFAhdk1? NFPMVJMzOzRzMkmzNS=>
MV4-11 NH7Pc5BCeG:ydH;zbZMhSXO|YYm= MljZPE8zPCCq Mnr6bY5lfWOnczDzbYdvcW[rY3HueEBidmRiZH;z[U1l\XCnbnTlcpQhWEGUUDDjcIVifmGpZTDhcoQh[WOldX31cIF1cW:wIH;mJJN2[i1{TjDEUmE> M3ziXVI{PDF{OUOx
MOLM-14 MoPQRZBweHSxc3nzJGF{e2G7 MX[4M|I1KGh? M2rDT4lv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C NFHHTFkzOzRzMkmzNS=>
SEM-K2 MXTBdI9xfG:|aYOgRZN{[Xl? NG\IPIc5NzJ2IHi= NE\zb2RqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? NHHwZpczOzRzMkmzNS=>
MV4-11 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXG3NkBp NXTaU21uUUN3ME2wMlU3KMLzIECuN{BvVQ>? MWWxPVY2PDRyOB?=
A375 M2j4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\pdVczKGh? Mo\vTWM2OD5iMUCgNFAxKG6P MYexPVY2PDRyOB?=

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Female NU/NU or severe combined immunodeficient mice implanted with MV4-11 cells
  • Formulation: Formulated in 22% hydroxypropyl-β-cyclodextrin
  • 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03735875 Recruiting Acute Myeloid Leukemia With FLT3/ITD Mutation|FLT3 Gene Mutation|FLT3 Internal Tandem Duplication|Recurrent Acute Myeloid Leukemia|Refractory Acute Leukemia M.D. Anderson Cancer Center|National Cancer Institute (NCI) January 25 2019 Phase 1|Phase 2
NCT03735875 Recruiting Acute Myeloid Leukemia With FLT3/ITD Mutation|FLT3 Gene Mutation|FLT3 Internal Tandem Duplication|Recurrent Acute Myeloid Leukemia|Refractory Acute Leukemia M.D. Anderson Cancer Center|National Cancer Institute (NCI) January 25 2019 Phase 1|Phase 2
NCT03723681 Recruiting Acute Myeloid Leukemia (AML) Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. November 5 2018 Phase 1
NCT03723681 Recruiting Acute Myeloid Leukemia (AML) Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. November 5 2018 Phase 1
NCT03661307 Recruiting Acute Myeloid Leukemia With FLT3/ITD Mutation|Blasts More Than 10 Percent of Bone Marrow Nucleated Cells|Blasts More Than 10 Percent of Peripheral Blood White Cells|Myelodysplastic Syndrome|Recurrent Acute Myeloid Leukemia|Recurrent Myelodysplastic Syndrome M.D. Anderson Cancer Center|National Cancer Institute (NCI) October 31 2018 Phase 1|Phase 2
NCT03661307 Recruiting Acute Myeloid Leukemia With FLT3/ITD Mutation|Blasts More Than 10 Percent of Bone Marrow Nucleated Cells|Blasts More Than 10 Percent of Peripheral Blood White Cells|Myelodysplastic Syndrome|Recurrent Acute Myeloid Leukemia|Recurrent Myelodysplastic Syndrome M.D. Anderson Cancer Center|National Cancer Institute (NCI) October 31 2018 Phase 1|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