Quizartinib (AC220)

For research use only. Not for use in humans.

Catalog No.S1526

54 publications

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 353 In stock
USD 210 In stock
USD 370 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Quizartinib (AC220) has been cited by 54 publications

Purity & Quality Control

Choose Selective FLT3 Inhibitors

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 Mm[zSpVv[3Srb36gRZN{[Xl? MkHsNE4yNTFyIN88US=> NG[zZmI{OCCvaX6= NEG2PWFmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? M{DhRVI{QTZ5MUe3
K562/ABCB1 M2fWWmZ2dmO2aX;uJGF{e2G7 NGn3dJAxNjFvMUCg{txO M16xZ|MxKG2rbh?= MWXlcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NUn1cmVLOjN7NkexO|c>
8226/MR20  MnLKSpVv[3Srb36gRZN{[Xl? MXmwMlEuOTBizszN MXmzNEBucW5? MnTX[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz Mn3WNlM6PjdzN{e=
K562/ABCG2 NXzZRWdxTnWwY4Tpc44hSXO|YYm= MlfhNE4yNTFyIN88US=> MluwN|AhdWmw M3LxSIVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MWCyN|k3PzF5Nx?=
MCF-7 FLV1000 M4HEeGtqdmG|ZTDBd5NigQ>? MoruNQKBmzNyINM1US=> NGPYWGo2KG2rbh?= NHW2NmJl\WO{ZXHz[ZMhYzF{NVndMWlCSVBicHjveI9t[WKnbHnu[{Bw\iCDQlPCNUBifCCLQ{WwJI9nKDNwMzFOwG0> M1;SbVI{QTZ5MUe3
MCF-7 FLV1000 NEW3XWNMcW6jc3WgRZN{[Xl? NFXNVG4x6oDVM{CgxtVO NVHEVW1rPSCvaX6= NVzFNpJH\GWlcnXhd4V{KFtzMkXJYU1KSUGSIIDoc5RwdGGkZXzpcochd2ZiQVLDRlIh[XRiSVO1NEBw\iByLkC3JO69VQ>? M{iyT|I{QTZ5MUe3
K562/ABCG2 MkLlR4VtdCCYaXHibYxqfHliQYPzZZl{ NVTQZoRYOC5zL{CuOU8yKML3TR?= NIDreng6PiCq Mluwd4Vve2m2aYrld{BMPTZ{L1HCR2czKGOnbHzzJJRwKG2rdH;4ZY51em:wZTD0c5BwfGWlYX9CpC=> M4XTXlI{QTZ5MUe3
8226/MR20 Mon5R4VtdCCYaXHibYxqfHliQYPzZZl{ NXjuVXNGOC5zINM1US=> NIHLeHM6PiCq MX\z[Y5{cXSrenXzJGs2PjJxQVLDS|Ih[2WubIOgeI8hdWm2b4jhcpRzd26nIITvdI91\WOjbtMg MoS5NlM6PjdzN{e=
HMC1.1 Mn3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDSTWM2OD1zNDDuUS=> MXWyN|Q6PzNzNx?=
HMC1.2 M1\hWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7zWlVJUUN3ME2xO|I4KG6P MmX4NlM1QTd|MUe=
p815 M1HXNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPkSHRbUUN3ME20OFUhdk1? MYWyN|Q6PzNzNx?=
Kasumi-1 M3fac2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[wTJhYUUN3ME2zOkBvVQ>? MoHYNlM1QTd|MUe=
M-07e + SCF NWrkTYJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1joPGlEPTB;N{egcm0> M3ju[VI{PDl5M{G3
EOL-1 M16wXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH4WG14UUN3ME2xJI5O MlHPNlM1QTd|MUe=
MV4;11 NFX4c5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1raU2lEPTB:IEGgcm0> MWWyN|Q6PzNzNx?=
MOLM14 NE\VSnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{KwPWlEPTB:IEGgcm0> NEjnbJQzOzR7N{OxOy=>
Pat.221 NUHvOHlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTZ5NTDuUS=> MWiyN|Q6PzNzNx?=
Pat.279 MmLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C4fmlEPTB;M{SzOEBvVQ>? NGfPNJIzOzR7N{OxOy=>
Pat.299 NWq4O4dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HjdmlEPTB;N{K0PEBvVQ>? NVW4ZZhUOjN2OUezNVc>
Pat.305 M3zPbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzDWI1uUUN3ME23NFc6KG6P M2D2cFI{PDl5M{G3
Pat.375 NV;4c3hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTVyMzDuUS=> MlHoNlM1QTd|MUe=
Pat.379 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LyWWlEPTB;OEC2JI5O NGjlXGkzOzR7N{OxOy=>
Pat.368 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{faTmlEPTB;MkewNEBvVQ>? MkfnNlM1QTd|MUe=
Pat.601 NV\kNpNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3T6fWlEPTB;MUG1N{BvVQ>? MniyNlM1QTd|MUe=
HMC1.1 NX7lcmtMSXCxcITvd4l{KEG|c3H5 NITm[YZKSzVyPUOxJI5O NEPkdI0zOzR7N{OxOy=>
p815 MUDBdI9xfG:|aYOgRZN{[Xl? NXHqZVlLUUN3ME2zOFEhdk1? NF35dmgzOzR7N{OxOy=>
Kasumi-1 M1HjdGFxd3C2b4Ppd{BCe3OjeR?= NGjqfmlKSzVyPU[3JI5O NFyxXpozOzR7N{OxOy=>
M-07e + SCF NWTObIczSXCxcITvd4l{KEG|c3H5 M3nzd2lEPTB;N{igcm0> M2LUOlI{PDl5M{G3
EOL-1 NIe4OIJCeG:ydH;zbZMhSXO|YYm= NH;KT|ZKSzVyPDCxJI5O MWqyN|Q6PzNzNx?=
MV4;11 NUjpOWJqSXCxcITvd4l{KEG|c3H5 NH:5O25KSzVyPUKgcm0> M17wRVI{PDl5M{G3
MOLM14 M{fBcmFxd3C2b4Ppd{BCe3OjeR?= MYDJR|UxRTNibl2= MWGyN|Q6PzNzNx?=
GIST822 M2TEc2Fxd3C2b4Ppd{BCe3OjeR?= NH\nVZRKSzVyPUGwPUBvVQ>? MYqyN|Q6PzNzNx?=
Pat.368 NXvsV21mSXCxcITvd4l{KEG|c3H5 MVnJR|UxRTJ7OUigcm0> NUf2VXZzOjN2OUezNVc>
Pat.601 MUXBdI9xfG:|aYOgRZN{[Xl? M2O3NGlEPTB;OEe2JI5O MljFNlM1QTd|MUe=
MV4-11 NWOxOmNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrwO|IhcA>? NETuV|JKSzVyPUCuN{BvVQ>? M3HNZVI{PDF{OUOx
MOLM-14 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nLelczKGh? MnvkTWM2OD1yLkGgcm0> M4PHR|I{PDF{OUOx
SEM-K2 NYfWN|VvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[5eoJ7PzJiaB?= MknwTWM2OD1yLkSgcm0> M4DtRVI{PDF{OUOx
RS4;11 NUHq[4c{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDaO|IhcA>? M2CxemlEPTB-MUCsNFAxKG6P M1;kSFI{PDF{OUOx
THP-1 M4W0Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfJO|IhcA>? NW\6foRMUUN3ME6xNEwxODBibl2= MlHvNlM1OTJ7M{G=
MV4-11 NIr1ZndCeG:ydH;zbZMhSXO|YYm= Mm\RPE8zPCCq NUL0UmM6cW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? M2TsUlI{PDF{OUOx
MOLM-14 NInGR2JCeG:ydH;zbZMhSXO|YYm= MUK4M|I1KGh? M{DZVolv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C NFfpO|QzOzRzMkmzNS=>
SEM-K2 MmiyRZBweHSxc3nzJGF{e2G7 NXSx[|ZrQC9{NDDo Mk\QbY5lfWOnczDzbYdvcW[rY3HueEBidmRiZH;z[U1l\XCnbnTlcpQhWEGUUDDjcIVifmGpZTDhcoQh[WOldX31cIF1cW:wIH;mJJN2[i1{TjDEUmE> NX;VVpVNOjN2MUK5N|E>
MV4-11 M1nlO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:3NkBp NY\yb5IzUUN3ME2wMlU3KMLzIECuN{BvVQ>? NISwXYkyQTZ3NESwPC=>
A375 M37LNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrTO2VWPzJiaB?= MnzqTWM2OD5iMUCgNFAxKG6P MUOxPVY2PDRyOB?=

... 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
Smiles CC(C)(C)C1=CC(=NO1)NC(=O)NC2=CC=C(C=C2)C3=C[N]4C(=N3)SC5=CC(=CC=C45)OCCN6CCOCC6

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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.

FLT3 Signaling Pathway Map

FLT3 Inhibitors with Unique Features

Related FLT3 Products

Tags: buy Quizartinib (AC220) | Quizartinib (AC220) supplier | purchase Quizartinib (AC220) | Quizartinib (AC220) cost | Quizartinib (AC220) manufacturer | order Quizartinib (AC220) | Quizartinib (AC220) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID