Quizartinib (AC220)

For research use only.

Catalog No.S1526

64 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 64 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 NXP0e2JHTnWwY4Tpc44hSXO|YYm= M{H1N|AvOS1zMDFOwG0> MYWzNEBucW5? MonG[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MY[yN|k3PzF5Nx?=
K562/ABCB1 M{j1dmZ2dmO2aX;uJGF{e2G7 MYqwMlEuOTBizszN MV6zNEBucW5? M4D5b4VvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MYCyN|k3PzF5Nx?=
8226/MR20  NX36UId7TnWwY4Tpc44hSXO|YYm= NXjHS4diOC5zLUGwJO69VQ>? MVmzNEBucW5? MXnlcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> M{TE[FI{QTZ5MUe3
K562/ABCG2 MkjNSpVv[3Srb36gRZN{[Xl? MXmwMlEuOTBizszN NGfDb3E{OCCvaX6= NYHIfHoy\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ M{PLRlI{QTZ5MUe3
MCF-7 FLV1000 MorJT4lv[XOnIFHzd4F6 MXSw5qCUOzBiwsXN NEXCTG42KG2rbh?= NFrRS|dl\WO{ZXHz[ZMhYzF{NVndMWlCSVBicHjveI9t[WKnbHnu[{Bw\iCDQlPCNUBifCCLQ{WwJI9nKDNwMzFOwG0> MXeyN|k3PzF5Nx?=
MCF-7 FLV1000 MVLLbY5ie2ViQYPzZZk> NWfVcWxvOOLCk{OwJOK2VQ>? MWm1JI1qdg>? NXzh[214\GWlcnXhd4V{KFtzMkXJYU1KSUGSIIDoc5RwdGGkZXzpcochd2ZiQVLDRlIh[XRiSVO1NEBw\iByLkC3JO69VQ>? NGm3UIYzOzl4N{G3Oy=>
K562/ABCG2 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfZM> NHi4boIxNjFxMD61M|EhyrWP MmTtPVYhcA>? MmjNd4Vve2m2aYrld{BMPTZ{L1HCR2czKGOnbHzzJJRwKG2rdH;4ZY51em:wZTD0c5BwfGWlYX9CpC=> MXSyN|k3PzF5Nx?=
8226/MR20 M2naeGNmdGxiVnnhZoltcXS7IFHzd4F6ew>? NVzGV2M3OC5zINM1US=> NVG3OWpzQTZiaB?= Mkm3d4Vve2m2aYrld{BMPTZ{L1HCR2czKGOnbHzzJJRwKG2rdH;4ZY51em:wZTD0c5BwfGWlYX9CpC=> MnHWNlM6PjdzN{e=
HMC1.1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnMN3lKSzVyPUG0JI5O NH;BZm8zOzR7N{OxOy=>
HMC1.2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\pcZNPUUN3ME2xO|I4KG6P NHL6W4UzOzR7N{OxOy=>
p815 NVHWSJBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjrWoZsUUN3ME20OFUhdk1? MXOyN|Q6PzNzNx?=
Kasumi-1 NVLyVYd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTN4IH7N NWDj[IVyOjN2OUezNVc>
M-07e + SCF NWnrbpRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2r2NGlEPTB;N{egcm0> Mli0NlM1QTd|MUe=
EOL-1 M3jqfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXuTWM2OD1zIH7N MVuyN|Q6PzNzNx?=
MV4;11 M4j4W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRCBzIH7N MXiyN|Q6PzNzNx?=
MOLM14 NVLt[VdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\MPWZKSzVyPDCxJI5O M1nOclI{PDl5M{G3
Pat.221 MmXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nzZmlEPTB;Nke1JI5O MmrnNlM1QTd|MUe=
Pat.279 M2THRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTN2M{Sgcm0> M4PZ[lI{PDl5M{G3
Pat.299 NWLtRYV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTLVY5KSzVyPUeyOFghdk1? MW[yN|Q6PzNzNx?=
Pat.305 NVPzNW1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUOyN2xqUUN3ME23NFc6KG6P M3LVe|I{PDl5M{G3
Pat.375 M33uVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUD3fmozUUN3ME21NFMhdk1? NUL4OolyOjN2OUezNVc>
Pat.379 NGDQNFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUn1[|g{UUN3ME24NFYhdk1? NHXFcFIzOzR7N{OxOy=>
Pat.368 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LGS2lEPTB;MkewNEBvVQ>? MX:yN|Q6PzNzNx?=
Pat.601 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTFzNUOgcm0> M2\3UlI{PDl5M{G3
HMC1.1 M2HycWFxd3C2b4Ppd{BCe3OjeR?= M2G2OGlEPTB;M{Ggcm0> M2nWUVI{PDl5M{G3
p815 M3mxXWFxd3C2b4Ppd{BCe3OjeR?= NGfYTZFKSzVyPUO0NUBvVQ>? NE\YN3QzOzR7N{OxOy=>
Kasumi-1 MV;BdI9xfG:|aYOgRZN{[Xl? NH7BOnBKSzVyPU[3JI5O MWmyN|Q6PzNzNx?=
M-07e + SCF MXHBdI9xfG:|aYOgRZN{[Xl? MYHJR|UxRTd6IH7N NH\LNGczOzR7N{OxOy=>
EOL-1 MlHlRZBweHSxc3nzJGF{e2G7 NEnReXZKSzVyPDCxJI5O MlvHNlM1QTd|MUe=
MV4;11 MWnBdI9xfG:|aYOgRZN{[Xl? NWLjdWhJUUN3ME2yJI5O NVT4RlJwOjN2OUezNVc>
MOLM14 MVPBdI9xfG:|aYOgRZN{[Xl? NIXvdZNKSzVyPUOgcm0> NGOyT2wzOzR7N{OxOy=>
GIST822 Mny0RZBweHSxc3nzJGF{e2G7 MmnMTWM2OD1zMEmgcm0> MX6yN|Q6PzNzNx?=
Pat.368 M3rKcmFxd3C2b4Ppd{BCe3OjeR?= MWrJR|UxRTJ7OUigcm0> MmDqNlM1QTd|MUe=
Pat.601 MVzBdI9xfG:|aYOgRZN{[Xl? NXSyVppIUUN3ME24O|Yhdk1? NVjCWYRIOjN2OUezNVc>
MV4-11 M4jVTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3zSlREPzJiaB?= NGfaOlFKSzVyPUCuN{BvVQ>? NXLYVppMOjN2MUK5N|E>
MOLM-14 M2[4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV63NkBp NETtU21KSzVyPUCuNUBvVQ>? MUmyN|QyOjl|MR?=
SEM-K2 NF\ld4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXYTlE4OiCq MY\JR|UxRTBwNDDuUS=> Ml\ENlM1OTJ7M{G=
RS4;11 NYjDeXdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPZU2VPPzJiaB?= NVHDTWc4UUN3ME6xNEwxODBibl2= NWT0b4NVOjN2MUK5N|E>
THP-1 NVPENFdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXy3NkBp Mn:wTWM2OD5zMDywNFAhdk1? MY[yN|QyOjl|MR?=
MV4-11 MnWyRZBweHSxc3nzJGF{e2G7 NWPMRYlVQC9{NDDo M4rMfolv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C MWqyN|QyOjl|MR?=
MOLM-14 MoD2RZBweHSxc3nzJGF{e2G7 MkPYPE8zPCCq MV\pcoR2[2W|IIPp[45q\mmlYX70JIFv\CCmb4PlMYRmeGWwZHXueEBRSVKSIHPs[YF3[WenIHHu[EBi[2O3bYXsZZRqd25ib3[gd5VjNTKQIFTORS=> MkXDNlM1OTJ7M{G=
SEM-K2 M1TIN2Fxd3C2b4Ppd{BCe3OjeR?= MonMPE8zPCCq MX\pcoR2[2W|IIPp[45q\mmlYX70JIFv\CCmb4PlMYRmeGWwZHXueEBRSVKSIHPs[YF3[WenIHHu[EBi[2O3bYXsZZRqd25ib3[gd5VjNTKQIFTORS=> M{TMU|I{PDF{OUOx
MV4-11 M{fTW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnDcFU4OiCq MWLJR|UxRTBwNU[gxtEhOC5|IH7N MofoNVk3PTR2MEi=
A375 NUHzZ|JzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWn0bIhPPzJiaB?= MkLJTWM2OD5iMUCgNFAxKG6P MVuxPVY2PDRyOB?=

... 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