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.

5 Customer Reviews

  • B. MOLM-14 cells were treated with PBS (control) or FLT3 inhibitor (100 nM) for 16 h, and were then stained for LC3B-FITC and analysed by flow cytometry. Histograms represent the percentages of LC3B-FITC medium fluorescence intensity (MFI) of cells treated with FLT3 inhibitor, normalized to PBS-treated cells (n=3 ± SEM). The FLT3 inhibitor is quizartinib.

    Oncogene, 2018, 37(6):787-797. Quizartinib (AC220) purchased from Selleck.

    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.

  • 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.

    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.

  • 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 MWDGeY5kfGmxbjDBd5NigQ>? NUK5WoNrOC5zLUGwJO69VQ>? NUH0cIFWOzBibXnu NIjaW4ZmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? M4XUcVI{QTZ5MUe3
K562/ABCB1 MX3GeY5kfGmxbjDBd5NigQ>? MWKwMlEuOTBizszN MlTMN|AhdWmw MXzlcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> Mk\uNlM6PjdzN{e=
8226/MR20  Mo[1SpVv[3Srb36gRZN{[Xl? M2TudVAvOS1zMDFOwG0> NXjDNIM{OzBibXnu MY\lcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> M2\uZlI{QTZ5MUe3
K562/ABCG2 MmnwSpVv[3Srb36gRZN{[Xl? NHPSeWMxNjFvMUCg{txO MX:zNEBucW5? NFjUfZFmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MnPxNlM6PjdzN{e=
MCF-7 FLV1000 NWjZNWRkU2mwYYPlJGF{e2G7 MUOw5qCUOzBiwsXN M1HDPVUhdWmw MnfW[IVkemWjc3XzJHsyOjWLXT3JRWFRKHCqb4TvcIFj\Wyrbnegc4YhSUKFQkGgZZQhUUN3MDDv[kA{NjNizszN MmLKNlM6PjdzN{e=
MCF-7 FLV1000 Ml60T4lv[XOnIFHzd4F6 NEfwWYQx6oDVM{CgxtVO MXO1JI1qdg>? MWLk[YNz\WG|ZYOgX|EzPUmfLVnBRXAheGixdH;sZYJmdGmwZzDv[kBCSkOEMjDheEBKSzVyIH;mJFAvODdizszN NID3SGczOzl4N{G3Oy=>
K562/ABCG2 MlXQR4VtdCCYaXHibYxqfHliQYPzZZl{ NFPKUHMxNjFxMD61M|EhyrWP MWW5OkBp NUHLZ2Zxe2Wwc3n0bZpmeyCNNU[yM2FDS0d{IHPlcIx{KHSxIH3peI95[W62cn;u[UB1d3CxdHXjZY7DqA>? MV6yN|k3PzF5Nx?=
8226/MR20 MWHD[YxtKF[rYXLpcIl1gSCDc4PhfZM> Mn;sNE4yKML3TR?= MofIPVYhcA>? MUjz[Y5{cXSrenXzJGs2PjJxQVLDS|Ih[2WubIOgeI8hdWm2b4jhcpRzd26nIITvdI91\WOjbtMg NWr1b5lMOjN7NkexO|c>
HMC1.1 Mnu3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTF2IH7N M3;2clI{PDl5M{G3
HMC1.2 MlnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvTdY9KSzVyPUG3Nlchdk1? NVzvbZVpOjN2OUezNVc>
p815 M{jp[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PEXmlEPTB;NES1JI5O NEK1dnIzOzR7N{OxOy=>
Kasumi-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTN4IH7N M1LKZlI{PDl5M{G3
M-07e + SCF NFH0Z|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLONmw5UUN3ME23O{BvVQ>? NHX6bIozOzR7N{OxOy=>
EOL-1 M{HaOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHqxfIRKSzVyPUGgcm0> NUeyeGdEOjN2OUezNVc>
MV4;11 NHfwU5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmxU|JKSzVyPDCxJI5O NYjmXnZMOjN2OUezNVc>
MOLM14 M1\ON2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRCBzIH7N MXKyN|Q6PzNzNx?=
Pat.221 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LQRWlEPTB;Nke1JI5O MljCNlM1QTd|MUe=
Pat.279 NX3YN203T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jIUmlEPTB;M{SzOEBvVQ>? MknoNlM1QTd|MUe=
Pat.299 NH3j[ZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfYeopKSzVyPUeyOFghdk1? NV7UWYJSOjN2OUezNVc>
Pat.305 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTdyN{mgcm0> M{\MUFI{PDl5M{G3
Pat.375 Mn:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4njfGlEPTB;NUCzJI5O Mm\5NlM1QTd|MUe=
Pat.379 Ml;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHsSpZKSzVyPUiwOkBvVQ>? NX\3R4tbOjN2OUezNVc>
Pat.368 Mmf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTJ5MECgcm0> MX:yN|Q6PzNzNx?=
Pat.601 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFzNUOgcm0> MV[yN|Q6PzNzNx?=
HMC1.1 NF\qN2VCeG:ydH;zbZMhSXO|YYm= MXfJR|UxRTNzIH7N MkjWNlM1QTd|MUe=
p815 MnflRZBweHSxc3nzJGF{e2G7 M1PLdGlEPTB;M{SxJI5O NUDFTmsxOjN2OUezNVc>
Kasumi-1 MUXBdI9xfG:|aYOgRZN{[Xl? M1TXZWlEPTB;Nkegcm0> M1fwR|I{PDl5M{G3
M-07e + SCF MV;BdI9xfG:|aYOgRZN{[Xl? M33wbGlEPTB;N{igcm0> NVPEdVZGOjN2OUezNVc>
EOL-1 M{XId2Fxd3C2b4Ppd{BCe3OjeR?= MVjJR|UxRCBzIH7N MmXiNlM1QTd|MUe=
MV4;11 NYDNT2w4SXCxcITvd4l{KEG|c3H5 NHqxVmhKSzVyPUKgcm0> NVWxTlNIOjN2OUezNVc>
MOLM14 NYHnOYoxSXCxcITvd4l{KEG|c3H5 MXTJR|UxRTNibl2= NWfkN49OOjN2OUezNVc>
GIST822 M3LwSWFxd3C2b4Ppd{BCe3OjeR?= NUG0boNwUUN3ME2xNFkhdk1? NYrmTGtrOjN2OUezNVc>
Pat.368 MkXaRZBweHSxc3nzJGF{e2G7 Mlj6TWM2OD1{OUm4JI5O MXGyN|Q6PzNzNx?=
Pat.601 MXXBdI9xfG:|aYOgRZN{[Xl? NHrKbXJKSzVyPUi3OkBvVQ>? M3HoR|I{PDl5M{G3
MV4-11 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVq3NkBp M1HsUmlEPTB;MD6zJI5O NEPvSXkzOzRzMkmzNS=>
MOLM-14 NWTzfJo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXm3NkBp MWTJR|UxRTBwMTDuUS=> MWeyN|QyOjl|MR?=
SEM-K2 M3\oOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTlO|IhcA>? NELNN|dKSzVyPUCuOEBvVQ>? M4TvU|I{PDF{OUOx
RS4;11 MonFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnTSnI4OiCq NF7nXXhKSzVyPkGwMFAxOCCwTR?= MkDwNlM1OTJ7M{G=
THP-1 NH;w[FNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVm3NkBp NXXO[FJGUUN3ME6xNEwxODBibl2= NV7qOnhXOjN2MUK5N|E>
MV4-11 NV\PXXk{SXCxcITvd4l{KEG|c3H5 NIL2TW05NzJ2IHi= M{fIWIlv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C NFqwNYIzOzRzMkmzNS=>
MOLM-14 M2nqZWFxd3C2b4Ppd{BCe3OjeR?= MYK4M|I1KGh? M2nQWYlv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C MoXDNlM1OTJ7M{G=
SEM-K2 MmrwRZBweHSxc3nzJGF{e2G7 NG\NblQ5NzJ2IHi= M4L4SYlv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C Mlr1NlM1OTJ7M{G=
MV4-11 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLxZVI4OiCq M2myZ2lEPTB;MD61OkDDuSByLkOgcm0> M1L2ZVE6PjV2NEC4
A375 NF\idnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX63NkBp M1fXXmlEPTB-IEGwJFAxOCCwTR?= MnTLNVk3PTR2MEi=

... 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(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

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
NCT03735875 Not yet recruiting Acute Myeloid Leukemia With FLT3/ITD Mutation|FLT3 Gene Mutation|FLT3 Internal Tandem Duplication|Recurrent Acute Myeloid Leukemia|Refractory Acute Leukemia M.D. Anderson Cancer Center|National Cancer Institute (NCI) March 31 2019 Phase 1|Phase 2
NCT03723681 Not yet recruiting Acute Myeloid Leukemia (AML) Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. October 2018 Phase 1
NCT03661307 Recruiting Acute Myeloid Leukemia With FLT3/ITD Mutation|Blasts More Than 10 Percent of Bone Marrow Nucleated Cells|Blasts More Than 10 Percent of Peripheral Blood White Cells|Myelodysplastic Syndrome|Recurrent Acute Myeloid Leukemia|Recurrent Myelodysplastic Syndrome M.D. Anderson Cancer Center|National Cancer Institute (NCI) October 31 2018 Phase 1|Phase 2
NCT03552029 Recruiting Acute Myeloid Leukemia Daiichi Sankyo Inc. August 27 2018 Phase 1
NCT03135054 Recruiting AML|FLT3-ITD Mutation The University of Hong Kong October 1 2017 Phase 2
NCT02984995 Completed Leukemia Myeloid Acute Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. December 2016 Phase 2

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 Products4

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