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.

Size Price Stock Quantity  
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.

4 Customer Reviews

  • Cotreatment with JQ1 and AC220 synergistically induces apoptosis of FLT3-ITD–expressing AML cells. MV4-11 cells were treated with the indicated concentrations of AC220 and/or JQ1 for 24 hours. At the end of treatment, immunoblot analyses were conducted as indicated. The numbers beneath the blots represent densitometry analysis conducted on representative blots.

    Mol Cancer Ther 2014 13(10), 2315-27. Quizartinib (AC220) purchased from Selleck.

    Crude membranes from High-Five insect cells expressing ABCB1 and MCF-7 FLV1000 cells expressing ABCG2 were incubated with 0–30 uM quizartinib for 5 minutes at 21–23°C in 50 mM Tris-HCl, pH 7.5 and 3–6 nM [125I]-IAAP (2200 Ci/mmole) was added. Representative autoradiograms from one experiment are shown in the upper panels; similar results were obtained in two additional experiments. In the lower panels, incorporation of [125I]-IAAP (from autoradiogram, Y-axis) into the ABCB1 and ABCG2 bands was plotted as a function of quizartinib concentration (X-axis). Quizartinib inhibited [125I]-IAAP binding to ABCB1 and ABCG2 with IC50’s of 3.3 uM and 0.07 uM, respectively, and the latter correspond to a therapeutically relevant plasma concentration. Values are from a representative experiment among three independent experiments.

    PLoS One 2013 8(8), e71266. Quizartinib (AC220) purchased from Selleck.

  • The effect of the FLT3 inhibitor AC220 (2nM) on the expression of MYC and E2F1 in MOLM-13 and MV4;11 cells. Cells were treated with vehicle and the FLT3 specific inhibitor AC220 for 24 hM, and then the mRNA and protein levels of MYC and E2F1 were tested.

    Leuk Lymphoma, 2017, 58(10):2426-2438. Quizartinib (AC220) purchased from Selleck.

    Effect of AC220 on the sensitivity of KB-C2 cells to paclitaxel. The figure showes the survival curves of cells at different concentrations of paclitaxel with or without AC220.  Cell viability was determined by MTT Assay.  KB-3-1 is epidermoid carcinoma cell line while KB-C2 is ABCB1 (P-gp) overexpressing drug (cholchicine) selected cell line. VERA (Verapamil) was used as a positive control of ABCB1 inhibitor.

    Quizartinib (AC220) purchased from Selleck.

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 MVrGeY5kfGmxbjDBd5NigQ>? Mn7lNE4yNTFyIN88US=> NX7n[|c5OzBibXnu NUnleIxZ\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NFfHSXUzOzl4N{G3Oy=>
K562/ABCB1 MVnGeY5kfGmxbjDBd5NigQ>? NUnnSZA4OC5zLUGwJO69VQ>? M2XpRlMxKG2rbh?= NWD4NW5L\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MVuyN|k3PzF5Nx?=
8226/MR20  NX\hZZB[TnWwY4Tpc44hSXO|YYm= NFHQS20xNjFvMUCg{txO M3nIOVMxKG2rbh?= NVzhXVVM\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ M3mzfVI{QTZ5MUe3
K562/ABCG2 MnG3SpVv[3Srb36gRZN{[Xl? MUWwMlEuOTBizszN NGDXVG8{OCCvaX6= NYf1TIo4\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NFnCc3EzOzl4N{G3Oy=>
MCF-7 FLV1000 NGfHWJJMcW6jc3WgRZN{[Xl? NFnz[Isx6oDVM{CgxtVO M1rT[|UhdWmw NETHVpFl\WO{ZXHz[ZMhYzF{NVndMWlCSVBicHjveI9t[WKnbHnu[{Bw\iCDQlPCNUBifCCLQ{WwJI9nKDNwMzFOwG0> MlXsNlM6PjdzN{e=
MCF-7 FLV1000 NWf3WVJ4U2mwYYPlJGF{e2G7 M3G1VlDjiJN|MDFCuW0> MU[1JI1qdg>? NIjOWFNl\WO{ZXHz[ZMhYzF{NVndMWlCSVBicHjveI9t[WKnbHnu[{Bw\iCDQlPCNkBifCCLQ{WwJI9nKDBwMEeg{txO MX2yN|k3PzF5Nx?=
K562/ABCG2 NGnqeGFE\WyuIG\pZYJqdGm2eTDBd5NigXN? Mo\GNE4yNzBwNT:xJOK2VQ>? M4e5clk3KGh? MlPDd4Vve2m2aYrld{BMPTZ{L1HCR2czKGOnbHzzJJRwKG2rdH;4ZY51em:wZTD0c5BwfGWlYX9CpC=> Ml\xNlM6PjdzN{e=
8226/MR20 NWTnRoxXS2WubDDWbYFjcWyrdImgRZN{[Xm| NGriUlExNjFiwsXN MX[5OkBp NUnIT|FXe2Wwc3n0bZpmeyCNNU[yM2FDS0d{IHPlcIx{KHSxIH3peI95[W62cn;u[UB1d3CxdHXjZY7DqA>? NUflemoxOjN7NkexO|c>
HMC1.1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjOXGRPUUN3ME2xOEBvVQ>? NFXRNlgzOzR7N{OxOy=>
HMC1.2 M{jkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlThTWM2OD1zN{K3JI5O MlXmNlM1QTd|MUe=
p815 MkPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jxNWlEPTB;NES1JI5O NFH3WpQzOzR7N{OxOy=>
Kasumi-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTN4IH7N MWWyN|Q6PzNzNx?=
M-07e + SCF MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3T4d2lEPTB;N{egcm0> Ml3iNlM1QTd|MUe=
EOL-1 NHfkNIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFibl2= NYnTWJpsOjN2OUezNVc>
MV4;11 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\RPFhKSzVyPDCxJI5O M1uwSFI{PDl5M{G3
MOLM14 NUPWbpJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HiRmlEPTB:IEGgcm0> MWWyN|Q6PzNzNx?=
Pat.221 NHnXPHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\qTWM2OD14N{Wgcm0> M2XxdlI{PDl5M{G3
Pat.279 M2L1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPKTWM2OD1|NEO0JI5O NI\TWFAzOzR7N{OxOy=>
Pat.299 M4rOZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[w[nk2UUN3ME23NlQ5KG6P MmnENlM1QTd|MUe=
Pat.305 NXr5fWcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHEdVBKSzVyPUewO|khdk1? MmPuNlM1QTd|MUe=
Pat.375 NUXqNmlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTVyMzDuUS=> NGrDb|gzOzR7N{OxOy=>
Pat.379 NF\wc2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXPTWM2OD16ME[gcm0> Mn\DNlM1QTd|MUe=
Pat.368 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjxdFhJUUN3ME2yO|AxKG6P MlnINlM1QTd|MUe=
Pat.601 MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlT5TWM2OD1zMUWzJI5O M1LlcVI{PDl5M{G3
HMC1.1 NHfiTGNCeG:ydH;zbZMhSXO|YYm= NEfyO2VKSzVyPUOxJI5O NEWzfHAzOzR7N{OxOy=>
p815 M2qzbGFxd3C2b4Ppd{BCe3OjeR?= NHy5[JFKSzVyPUO0NUBvVQ>? M1jLdlI{PDl5M{G3
Kasumi-1 M13lR2Fxd3C2b4Ppd{BCe3OjeR?= M2rIWGlEPTB;Nkegcm0> MlXqNlM1QTd|MUe=
M-07e + SCF MojlRZBweHSxc3nzJGF{e2G7 MW\JR|UxRTd6IH7N Ml7oNlM1QTd|MUe=
EOL-1 NHPrcVhCeG:ydH;zbZMhSXO|YYm= MW\JR|UxRCBzIH7N NUO0NG1NOjN2OUezNVc>
MV4;11 MlHJRZBweHSxc3nzJGF{e2G7 MUDJR|UxRTJibl2= MX6yN|Q6PzNzNx?=
MOLM14 M1TKfWFxd3C2b4Ppd{BCe3OjeR?= NGixV3BKSzVyPUOgcm0> Mkf1NlM1QTd|MUe=
GIST822 NIfJXW9CeG:ydH;zbZMhSXO|YYm= NXfFN5BCUUN3ME2xNFkhdk1? NGnnV24zOzR7N{OxOy=>
Pat.368 Mkm2RZBweHSxc3nzJGF{e2G7 M2q4WGlEPTB;Mkm5PEBvVQ>? NF63UJozOzR7N{OxOy=>
Pat.601 NWP0V2lmSXCxcITvd4l{KEG|c3H5 MYfJR|UxRTh5NjDuUS=> MVmyN|Q6PzNzNx?=
MV4-11 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfBc284OiCq NEfI[nRKSzVyPUCuN{BvVQ>? M1y5clI{PDF{OUOx
MOLM-14 NELQOmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml2yO|IhcA>? MWXJR|UxRTBwMTDuUS=> NUjFfo5VOjN2MUK5N|E>
SEM-K2 NGrNVGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV23NkBp NFSwcJFKSzVyPUCuOEBvVQ>? MljHNlM1OTJ7M{G=
RS4;11 MnLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HOXVczKGh? M1fpN2lEPTB-MUCsNFAxKG6P NHniXXczOzRzMkmzNS=>
THP-1 M1v3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYS3NkBp MXfJR|UxRjFyLECwNEBvVQ>? MVGyN|QyOjl|MR?=
MV4-11 NX3UZWZiSXCxcITvd4l{KEG|c3H5 M{fZT|gwOjRiaB?= MoXubY5lfWOnczDzbYdvcW[rY3HueEBidmRiZH;z[U1l\XCnbnTlcpQhWEGUUDDjcIVifmGpZTDhcoQh[WOldX31cIF1cW:wIH;mJJN2[i1{TjDEUmE> M4jPTlI{PDF{OUOx
MOLM-14 NVX5[Xk5SXCxcITvd4l{KEG|c3H5 NYTwe5BLQC9{NDDo NHzQUlFqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? MYKyN|QyOjl|MR?=
SEM-K2 NU[2fVUzSXCxcITvd4l{KEG|c3H5 M2TGVVgwOjRiaB?= MWnpcoR2[2W|IIPp[45q\mmlYX70JIFv\CCmb4PlMYRmeGWwZHXueEBRSVKSIHPs[YF3[WenIHHu[EBi[2O3bYXsZZRqd25ib3[gd5VjNTKQIFTORS=> NGTxXJAzOzRzMkmzNS=>
MV4-11 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDXO|IhcA>? NWPlTmlrUUN3ME2wMlU3KMLzIECuN{BvVQ>? MWixPVY2PDRyOB?=
A375 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\VblJQPzJiaB?= NGj2TopKSzVyPjCxNEAxODBibl2= MUixPVY2PDRyOB?=

... Click to View More Cell Line Experimental Data

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:
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

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 (g) = Concentration (mol/L) × Volume (L) × 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02984995 Recruiting Leukemia, Myeloid, Acute Daiichi Sankyo Co., Ltd.|Daiichi Sankyo Inc. December 2016 --
NCT02668653 Recruiting Acute Myeloid Leukemia|Leukemia Daiichi Sankyo Inc. September 2016 Phase 3
NCT02834390 Recruiting Acute Myeloid Leukemia Daiichi Sankyo Co., Ltd.|Daiichi Sankyo Inc. July 2016 Phase 1
NCT02675478 Recruiting Relapsed AML|Refractory AML Daiichi Sankyo Co., Ltd.|Daiichi Sankyo Inc. February 2016 Phase 1
NCT02272478 Recruiting Acute Myeloid Leukaemia|Myelodysplastic Syndrome Cardiff University|Cancer Research UK October 2014 Phase 3
NCT02039726 Recruiting AML Daiichi Sankyo Inc. April 2014 Phase 3

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