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 36 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 M17XPGZ2dmO2aX;uJGF{e2G7 MW[wMlEuOTBizszN M4SxV|MxKG2rbh?= NYLIbFNL\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NUDnXIdnOjN7NkexO|c>
K562/ABCB1 MYjGeY5kfGmxbjDBd5NigQ>? NYPwWFRDOC5zLUGwJO69VQ>? MlzlN|AhdWmw Ml;K[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NV;pcXlwOjN7NkexO|c>
8226/MR20  NXKzOm5xTnWwY4Tpc44hSXO|YYm= MVmwMlEuOTBizszN MoPEN|AhdWmw M4DX[4VvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? Mn7XNlM6PjdzN{e=
K562/ABCG2 Mn3lSpVv[3Srb36gRZN{[Xl? MUewMlEuOTBizszN NFzVbVY{OCCvaX6= M2LNN4VvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? M2X6[VI{QTZ5MUe3
MCF-7 FLV1000 MnLXT4lv[XOnIFHzd4F6 MoP1NQKBmzNyINM1US=> MVO1JI1qdg>? M2\SWYRm[3KnYYPld{BcOTJ3SW2tTWFCWCCyaH;0c4xi[mWuaX7nJI9nKEGEQ1KxJIF1KEmFNUCgc4YhOy5|IN88US=> M2fs[FI{QTZ5MUe3
MCF-7 FLV1000 NVfv[3czU2mwYYPlJGF{e2G7 MmTKNQKBmzNyINM1US=> MY[1JI1qdg>? M{TMeIRm[3KnYYPld{BcOTJ3SW2tTWFCWCCyaH;0c4xi[mWuaX7nJI9nKEGEQ1KyJIF1KEmFNUCgc4YhOC5yNzFOwG0> NIjTW3MzOzl4N{G3Oy=>
K562/ABCG2 MoTaR4VtdCCYaXHibYxqfHliQYPzZZl{ NIjSNJoxNjFxMD61M|EhyrWP M1HSOVk3KGh? NInBR4h{\W6|aYTpfoV{KEt3NkKvRWJETzJiY3XscJMhfG9ibXn0c5hidnS{b37lJJRweG:2ZXPhcuKh NETkR3EzOzl4N{G3Oy=>
8226/MR20 MU\D[YxtKF[rYXLpcIl1gSCDc4PhfZM> NH3WN2YxNjFiwsXN MUC5OkBp M4fnU5NmdnOrdHn6[ZMhUzV4Mj;BRmNIOiClZXzsd{B1dyCvaYTvfIFvfHKxbnWgeI9xd3SnY3HuxsA> MoGwNlM6PjdzN{e=
HMC1.1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTF2IH7N Ml:xNlM1QTd|MUe=
HMC1.2 NGnEb|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTF5Mkegcm0> NXHDe|VNOjN2OUezNVc>
p815 MoDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorkTWM2OD12NEWgcm0> M3LhNlI{PDl5M{G3
Kasumi-1 M1ruOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\tdmlEPTB;M{[gcm0> M2q0XVI{PDl5M{G3
M-07e + SCF M4SxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;n[G9KSzVyPUe3JI5O NEn0dWgzOzR7N{OxOy=>
EOL-1 M3\qeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2n3NmlEPTB;MTDuUS=> MV[yN|Q6PzNzNx?=
MV4;11 NEi1TJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4KzS2lEPTB:IEGgcm0> M4K2c|I{PDl5M{G3
MOLM14 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPkTWM2ODxiMTDuUS=> NVzWOVNKOjN2OUezNVc>
Pat.221 NXrCfmVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTZ5NTDuUS=> M3nmeVI{PDl5M{G3
Pat.279 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HHdWlEPTB;M{SzOEBvVQ>? MUOyN|Q6PzNzNx?=
Pat.299 NXuzWoRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvOXodkUUN3ME23NlQ5KG6P M{X3PFI{PDl5M{G3
Pat.305 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIeyfZJKSzVyPUewO|khdk1? Moj1NlM1QTd|MUe=
Pat.375 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\GUWVKSzVyPUWwN{BvVQ>? M{Kw[|I{PDl5M{G3
Pat.379 MlfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPvTWM2OD16ME[gcm0> MmXtNlM1QTd|MUe=
Pat.368 NYfvc2V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;ObotKSzVyPUK3NFAhdk1? NYTK[llJOjN2OUezNVc>
Pat.601 NVzW[ZhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7mVnZKSzVyPUGxOVMhdk1? MX[yN|Q6PzNzNx?=
HMC1.1 M3m0XWFxd3C2b4Ppd{BCe3OjeR?= M1TtXmlEPTB;M{Ggcm0> MYeyN|Q6PzNzNx?=
p815 NID4[HlCeG:ydH;zbZMhSXO|YYm= M4\VS2lEPTB;M{SxJI5O MYqyN|Q6PzNzNx?=
Kasumi-1 NHrPTIRCeG:ydH;zbZMhSXO|YYm= NV\3eWd1UUN3ME22O{BvVQ>? NX7IOFVCOjN2OUezNVc>
M-07e + SCF M2m5VmFxd3C2b4Ppd{BCe3OjeR?= Mn;ITWM2OD15ODDuUS=> NGKwT2UzOzR7N{OxOy=>
EOL-1 NUnkNnRNSXCxcITvd4l{KEG|c3H5 MnXCTWM2ODxiMTDuUS=> NYnD[3diOjN2OUezNVc>
MV4;11 M325RWFxd3C2b4Ppd{BCe3OjeR?= NHTSS|NKSzVyPUKgcm0> MoHoNlM1QTd|MUe=
MOLM14 M4TPSWFxd3C2b4Ppd{BCe3OjeR?= MkDITWM2OD1|IH7N M4C5XlI{PDl5M{G3
GIST822 NUSzeZRLSXCxcITvd4l{KEG|c3H5 MonkTWM2OD1zMEmgcm0> M4O2[FI{PDl5M{G3
Pat.368 NFmyfpJCeG:ydH;zbZMhSXO|YYm= M4DPfmlEPTB;Mkm5PEBvVQ>? NVPEPXk6OjN2OUezNVc>
Pat.601 NYrIVlc1SXCxcITvd4l{KEG|c3H5 M4jCe2lEPTB;OEe2JI5O M3XzS|I{PDl5M{G3
MV4-11 M2PxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7lU|M4OiCq M4\4[2lEPTB;MD6zJI5O MWeyN|QyOjl|MR?=
MOLM-14 NHnwWnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjTOlF3PzJiaB?= NX31XXdrUUN3ME2wMlEhdk1? MYGyN|QyOjl|MR?=
SEM-K2 M3P3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL5O|IhcA>? M2m0O2lEPTB;MD60JI5O NFKwZlQzOzRzMkmzNS=>
RS4;11 NIH3Tm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoH0O|IhcA>? M1f2UWlEPTB-MUCsNFAxKG6P M4q1XVI{PDF{OUOx
THP-1 M1nRPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIH4e|M4OiCq MXjJR|UxRjFyLECwNEBvVQ>? NEfrcHozOzRzMkmzNS=>
MV4-11 M1rSPGFxd3C2b4Ppd{BCe3OjeR?= M17jWVgwOjRiaB?= NX20WXV{cW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? M4PXUVI{PDF{OUOx
MOLM-14 NEi3cpFCeG:ydH;zbZMhSXO|YYm= MnTOPE8zPCCq NFXWVoNqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? NFrsfGQzOzRzMkmzNS=>
SEM-K2 Mn76RZBweHSxc3nzJGF{e2G7 NHL5OpU5NzJ2IHi= NUjNeotZcW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? M2\KUFI{PDF{OUOx
MV4-11 NEL2cZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrGd|lyPzJiaB?= M17SfGlEPTB;MD61OkDDuSByLkOgcm0> M{XnU|E6PjV2NEC4
A375 MkjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nFRVczKGh? NI\4R4hKSzVyPjCxNEAxODBibl2= Mm\4NVk3PTR2MEi=

... 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 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
NCT01565668 Completed Drug: AC220 Leukemia Myeloid Acute Daiichi Sankyo Inc.|Ambit Biosciences Corporation April 2012 Phase 2
NCT01049893 Completed Drug: Compound AC220 Solid Tumors Daiichi Sankyo Inc. January 2010 Phase 1
NCT00989261 Completed Drug: Compound AC220 Acute Myeloid Leukemia Daiichi Sankyo Inc. November 2009 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