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
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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.

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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 MkLxSpVv[3Srb36gRZN{[Xl? MYewMlEuOTBizszN NVSzUlhLOzBibXnu NXq1dWVz\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MUmyN|k3PzF5Nx?=
K562/ABCB1 MUHGeY5kfGmxbjDBd5NigQ>? M3yxSVAvOS1zMDFOwG0> NIDJRYM{OCCvaX6= M2LaPIVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MWCyN|k3PzF5Nx?=
8226/MR20  NEXwTZlHfW6ldHnvckBCe3OjeR?= Ml;UNE4yNTFyIN88US=> MVmzNEBucW5? NXfTV3Fm\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MnHTNlM6PjdzN{e=
K562/ABCG2 M3q5VmZ2dmO2aX;uJGF{e2G7 M3juZVAvOS1zMDFOwG0> NGn2b|M{OCCvaX6= MXTlcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> M4nqTFI{QTZ5MUe3
MCF-7 FLV1000 MV3LbY5ie2ViQYPzZZk> MVWw5qCUOzBiwsXN MYW1JI1qdg>? NH3hWpNl\WO{ZXHz[ZMhYzF{NVndMWlCSVBicHjveI9t[WKnbHnu[{Bw\iCDQlPCNUBifCCLQ{WwJI9nKDNwMzFOwG0> NGqzWpQzOzl4N{G3Oy=>
MCF-7 FLV1000 M{HudmtqdmG|ZTDBd5NigQ>? MoT5NQKBmzNyINM1US=> MlWzOUBucW5? NIPjcI9l\WO{ZXHz[ZMhYzF{NVndMWlCSVBicHjveI9t[WKnbHnu[{Bw\iCDQlPCNkBifCCLQ{WwJI9nKDBwMEeg{txO MWGyN|k3PzF5Nx?=
K562/ABCG2 NFvpW5lE\WyuIG\pZYJqdGm2eTDBd5NigXN? MkLhNE4yNzBwNT:xJOK2VQ>? NEC2WWE6PiCq MnnNd4Vve2m2aYrld{BMPTZ{L1HCR2czKGOnbHzzJJRwKG2rdH;4ZY51em:wZTD0c5BwfGWlYX9CpC=> MWGyN|k3PzF5Nx?=
8226/MR20 NHvoemVE\WyuIG\pZYJqdGm2eTDBd5NigXN? Ml;qNE4yKML3TR?= NUDFNpBJQTZiaB?= NF3wVIp{\W6|aYTpfoV{KEt3NkKvRWJETzJiY3XscJMhfG9ibXn0c5hidnS{b37lJJRweG:2ZXPhcuKh MUWyN|k3PzF5Nx?=
HMC1.1 M2K5Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIP0cXdKSzVyPUG0JI5O NH\DWXIzOzR7N{OxOy=>
HMC1.2 NUPhZ|RbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGL6TIpKSzVyPUG3Nlchdk1? MWOyN|Q6PzNzNx?=
p815 M4[3V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPZOGxCUUN3ME20OFUhdk1? NISzSXMzOzR7N{OxOy=>
Kasumi-1 MlPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HETGlEPTB;M{[gcm0> NHy0dVYzOzR7N{OxOy=>
M-07e + SCF MmjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHOTWM2OD15NzDuUS=> MWiyN|Q6PzNzNx?=
EOL-1 M1HL[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFibl2= MnT4NlM1QTd|MUe=
MV4;11 M3PiTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRCBzIH7N NHL5Z2gzOzR7N{OxOy=>
MOLM14 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXhO3dKSzVyPDCxJI5O M3fBR|I{PDl5M{G3
Pat.221 MkDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELqfllKSzVyPU[3OUBvVQ>? NXTaVGtlOjN2OUezNVc>
Pat.279 NIjmS|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13nOGlEPTB;M{SzOEBvVQ>? MmeyNlM1QTd|MUe=
Pat.299 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37ldWlEPTB;N{K0PEBvVQ>? MWeyN|Q6PzNzNx?=
Pat.305 Ml7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPPW|RKSzVyPUewO|khdk1? NHnae|EzOzR7N{OxOy=>
Pat.375 NGXKb4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTVyMzDuUS=> NYPMPXNUOjN2OUezNVc>
Pat.379 M2W0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTUTWM2OD16ME[gcm0> NYj1Zoc6OjN2OUezNVc>
Pat.368 NIXIXmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzsTWM2OD1{N{CwJI5O M322[VI{PDl5M{G3
Pat.601 M1nJVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[4VVczUUN3ME2xNVU{KG6P MlrSNlM1QTd|MUe=
HMC1.1 NYXt[IR5SXCxcITvd4l{KEG|c3H5 NIfT[I5KSzVyPUOxJI5O MVuyN|Q6PzNzNx?=
p815 MYLBdI9xfG:|aYOgRZN{[Xl? M4LYW2lEPTB;M{SxJI5O NYXCV|V{OjN2OUezNVc>
Kasumi-1 MonFRZBweHSxc3nzJGF{e2G7 MXHJR|UxRTZ5IH7N Ml7SNlM1QTd|MUe=
M-07e + SCF NGrGTYJCeG:ydH;zbZMhSXO|YYm= M1vTUWlEPTB;N{igcm0> M163cVI{PDl5M{G3
EOL-1 NH\GOolCeG:ydH;zbZMhSXO|YYm= MWPJR|UxRCBzIH7N NEfxVGYzOzR7N{OxOy=>
MV4;11 M3;obWFxd3C2b4Ppd{BCe3OjeR?= M1PGNWlEPTB;MjDuUS=> NUfa[WRjOjN2OUezNVc>
MOLM14 NX\pe5lYSXCxcITvd4l{KEG|c3H5 NXu1e5h4UUN3ME2zJI5O MkDzNlM1QTd|MUe=
GIST822 M1voSGFxd3C2b4Ppd{BCe3OjeR?= NF60OHBKSzVyPUGwPUBvVQ>? MUKyN|Q6PzNzNx?=
Pat.368 MoT4RZBweHSxc3nzJGF{e2G7 MmroTWM2OD1{OUm4JI5O NHjDd3ozOzR7N{OxOy=>
Pat.601 NUnuellsSXCxcITvd4l{KEG|c3H5 MV7JR|UxRTh5NjDuUS=> M1K2XlI{PDl5M{G3
MV4-11 MnezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV63NkBp MWjJR|UxRTBwMzDuUS=> NWLWWms1OjN2MUK5N|E>
MOLM-14 M1TmWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfmPIpHPzJiaB?= M4nMSWlEPTB;MD6xJI5O M1H5SFI{PDF{OUOx
SEM-K2 MlWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXUO|IhcA>? M1zUemlEPTB;MD60JI5O M13HW|I{PDF{OUOx
RS4;11 M2LtcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXm3NkBp NFr4OI9KSzVyPkGwMFAxOCCwTR?= MVWyN|QyOjl|MR?=
THP-1 MnXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\pO|IhcA>? NIXad4RKSzVyPkGwMFAxOCCwTR?= M{TaWVI{PDF{OUOx
MV4-11 MVfBdI9xfG:|aYOgRZN{[Xl? MVi4M|I1KGh? NH:5W2dqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? MmT0NlM1OTJ7M{G=
MOLM-14 NYLRepVySXCxcITvd4l{KEG|c3H5 NHnhR5g5NzJ2IHi= MnPXbY5lfWOnczDzbYdvcW[rY3HueEBidmRiZH;z[U1l\XCnbnTlcpQhWEGUUDDjcIVifmGpZTDhcoQh[WOldX31cIF1cW:wIH;mJJN2[i1{TjDEUmE> M{PoblI{PDF{OUOx
SEM-K2 MYXBdI9xfG:|aYOgRZN{[Xl? NGHJcI05NzJ2IHi= NX20Zm9TcW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? MVWyN|QyOjl|MR?=
MV4-11 NULGeHYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvKN5Q4OiCq MkmzTWM2OD1yLkW2JOKyKDBwMzDuUS=> MVmxPVY2PDRyOB?=
A375 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInyc444OiCq MV;JR|UxRiBzMDCwNFAhdk1? M4HjflE6PjV2NEC4

... 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

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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
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
NCT03723681 Not yet recruiting Acute Myeloid Leukemia (AML) Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. October 2018 Phase 1
NCT02984995 Completed Leukemia Myeloid Acute Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. December 2016 Phase 2
NCT02668653 Recruiting Acute Myeloid Leukemia|Leukemia Daiichi Sankyo Inc. September 2016 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

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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