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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In DMSO USD 353 In stock
USD 210 In stock
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USD 970 In stock
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Cited by 40 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 NITrSXlHfW6ldHnvckBCe3OjeR?= MWGwMlEuOTBizszN MmTjN|AhdWmw NYP5Xplx\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MVGyN|k3PzF5Nx?=
K562/ABCB1 MXfGeY5kfGmxbjDBd5NigQ>? MWOwMlEuOTBizszN NInoV|g{OCCvaX6= MkL6[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NYTzc3JKOjN7NkexO|c>
8226/MR20  NFrzRZFHfW6ldHnvckBCe3OjeR?= MX[wMlEuOTBizszN Mlr6N|AhdWmw M4HQeoVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? Ml:2NlM6PjdzN{e=
K562/ABCG2 M4XkdGZ2dmO2aX;uJGF{e2G7 NGDrU5QxNjFvMUCg{txO NFfRXFI{OCCvaX6= Mnrw[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NY\WSZE1OjN7NkexO|c>
MCF-7 FLV1000 MknqT4lv[XOnIFHzd4F6 NF;FXJEx6oDVM{CgxtVO MmP6OUBucW5? MUHk[YNz\WG|ZYOgX|EzPUmfLVnBRXAheGixdH;sZYJmdGmwZzDv[kBCSkOEMTDheEBKSzVyIH;mJFMvOyEQvF2= NGPzd28zOzl4N{G3Oy=>
MCF-7 FLV1000 NXLRU2JYU2mwYYPlJGF{e2G7 NHW0b48x6oDVM{CgxtVO M1PRSlUhdWmw MV3k[YNz\WG|ZYOgX|EzPUmfLVnBRXAheGixdH;sZYJmdGmwZzDv[kBCSkOEMjDheEBKSzVyIH;mJFAvODdizszN NHrmNYQzOzl4N{G3Oy=>
K562/ABCG2 MkDqR4VtdCCYaXHibYxqfHliQYPzZZl{ NHfoSJkxNjFxMD61M|EhyrWP NV[xdXE3QTZiaB?= MoHwd4Vve2m2aYrld{BMPTZ{L1HCR2czKGOnbHzzJJRwKG2rdH;4ZY51em:wZTD0c5BwfGWlYX9CpC=> M{ezNVI{QTZ5MUe3
8226/MR20 MUnD[YxtKF[rYXLpcIl1gSCDc4PhfZM> M3nablAvOSEEtV2= NYq5ZVBsQTZiaB?= NHfzdJN{\W6|aYTpfoV{KEt3NkKvRWJETzJiY3XscJMhfG9ibXn0c5hidnS{b37lJJRweG:2ZXPhcuKh MoLqNlM6PjdzN{e=
HMC1.1 MkHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLFTWM2OD1zNDDuUS=> MmDONlM1QTd|MUe=
HMC1.2 M2H1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDG[HNKSzVyPUG3Nlchdk1? NHfmeFkzOzR7N{OxOy=>
p815 M1L3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrqWWlKSzVyPUS0OUBvVQ>? MkHsNlM1QTd|MUe=
Kasumi-1 Ml3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTN4IH7N Mmr5NlM1QTd|MUe=
M-07e + SCF MmHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlT3TWM2OD15NzDuUS=> NGjKTFczOzR7N{OxOy=>
EOL-1 NXzzOmJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTBTWM2OD1zIH7N MW[yN|Q6PzNzNx?=
MV4;11 NXu1PHFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHO1ZXRKSzVyPDCxJI5O M3nJTVI{PDl5M{G3
MOLM14 NIXOdmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7OO4tHUUN3MEygNUBvVQ>? M2P1fFI{PDl5M{G3
Pat.221 MojiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XDUmlEPTB;Nke1JI5O NUTiUIRGOjN2OUezNVc>
Pat.279 Mn3PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\oR2lEPTB;M{SzOEBvVQ>? M3KwdFI{PDl5M{G3
Pat.299 MlX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLT[G9KSzVyPUeyOFghdk1? NUWwUoxVOjN2OUezNVc>
Pat.305 M1LqeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33PeWlEPTB;N{C3PUBvVQ>? NIHSU4ozOzR7N{OxOy=>
Pat.375 MkD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml:0TWM2OD13MEOgcm0> MUiyN|Q6PzNzNx?=
Pat.379 Mm\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\oTWM2OD16ME[gcm0> M1m5O|I{PDl5M{G3
Pat.368 NGntOmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[4colKSzVyPUK3NFAhdk1? MlLkNlM1QTd|MUe=
Pat.601 NHvUeJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnSfmJKSzVyPUGxOVMhdk1? MXWyN|Q6PzNzNx?=
HMC1.1 MlG4RZBweHSxc3nzJGF{e2G7 M3vQV2lEPTB;M{Ggcm0> NHLDWmozOzR7N{OxOy=>
p815 MlnWRZBweHSxc3nzJGF{e2G7 MnvVTWM2OD1|NEGgcm0> NF[zW5UzOzR7N{OxOy=>
Kasumi-1 M2\ydWFxd3C2b4Ppd{BCe3OjeR?= NULLfoM5UUN3ME22O{BvVQ>? NVK5[nF2OjN2OUezNVc>
M-07e + SCF NIr6bYVCeG:ydH;zbZMhSXO|YYm= MWDJR|UxRTd6IH7N MWGyN|Q6PzNzNx?=
EOL-1 MWnBdI9xfG:|aYOgRZN{[Xl? NVzRU5FjUUN3MEygNUBvVQ>? NH3ZSVEzOzR7N{OxOy=>
MV4;11 M3;HfmFxd3C2b4Ppd{BCe3OjeR?= Mn\4TWM2OD1{IH7N MYmyN|Q6PzNzNx?=
MOLM14 NGPTWIlCeG:ydH;zbZMhSXO|YYm= MnzjTWM2OD1|IH7N NHf5XJkzOzR7N{OxOy=>
GIST822 M1\jUGFxd3C2b4Ppd{BCe3OjeR?= M3;hemlEPTB;MUC5JI5O MUCyN|Q6PzNzNx?=
Pat.368 NYXWbos{SXCxcITvd4l{KEG|c3H5 MoHuTWM2OD1{OUm4JI5O MXWyN|Q6PzNzNx?=
Pat.601 Mny4RZBweHSxc3nzJGF{e2G7 NE\obZZKSzVyPUi3OkBvVQ>? NH;XTFEzOzR7N{OxOy=>
MV4-11 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DDcVczKGh? M4LoPWlEPTB;MD6zJI5O MmnQNlM1OTJ7M{G=
MOLM-14 MmnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33USFczKGh? M2TnbGlEPTB;MD6xJI5O MlqwNlM1OTJ7M{G=
SEM-K2 M1XWOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXuO|IhcA>? NYLxZ2x[UUN3ME2wMlQhdk1? MmftNlM1OTJ7M{G=
RS4;11 M3fSbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2GySlczKGh? NXHhUokzUUN3ME6xNEwxODBibl2= NFr1R3kzOzRzMkmzNS=>
THP-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TIZlczKGh? M{PVTGlEPTB-MUCsNFAxKG6P MWWyN|QyOjl|MR?=
MV4-11 MnSyRZBweHSxc3nzJGF{e2G7 M2nDOVgwOjRiaB?= MXHpcoR2[2W|IIPp[45q\mmlYX70JIFv\CCmb4PlMYRmeGWwZHXueEBRSVKSIHPs[YF3[WenIHHu[EBi[2O3bYXsZZRqd25ib3[gd5VjNTKQIFTORS=> NXTDWlJJOjN2MUK5N|E>
MOLM-14 NH\kOFZCeG:ydH;zbZMhSXO|YYm= NVXmc3c1QC9{NDDo MoCybY5lfWOnczDzbYdvcW[rY3HueEBidmRiZH;z[U1l\XCnbnTlcpQhWEGUUDDjcIVifmGpZTDhcoQh[WOldX31cIF1cW:wIH;mJJN2[i1{TjDEUmE> NFTF[JMzOzRzMkmzNS=>
SEM-K2 NGXLb5RCeG:ydH;zbZMhSXO|YYm= MkXOPE8zPCCq NXfHV2U4cW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? M1nIRVI{PDF{OUOx
MV4-11 NFTk[|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fzPFczKGh? MXfJR|UxRTBwNU[gxtEhOC5|IH7N NG[3dVYyQTZ3NESwPC=>
A375 M17rXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY[3NkBp MUHJR|UxRiBzMDCwNFAhdk1? NIDUU5YyQTZ3NESwPC=>

... 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
  • 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02984995 Completed Drug: Quizartinib Leukemia Myeloid Acute Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. December 2016 Phase 2
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