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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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. 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 NGfSTHlHfW6ldHnvckBCe3OjeR?= MU[wMlEuOTBizszN MoXwN|AhdWmw NYPk[5FL\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NGWybIwzOzl4N{G3Oy=>
K562/ABCB1 MmfKSpVv[3Srb36gRZN{[Xl? NYTXcVliOC5zLUGwJO69VQ>? MXWzNEBucW5? M4n2[IVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NWq5RYF4OjN7NkexO|c>
8226/MR20  NXPGOmJVTnWwY4Tpc44hSXO|YYm= MWKwMlEuOTBizszN M{\TUlMxKG2rbh?= NVPHe3I1\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MYGyN|k3PzF5Nx?=
K562/ABCG2 M1fz[mZ2dmO2aX;uJGF{e2G7 MWGwMlEuOTBizszN NYe0UJZxOzBibXnu M37ZNoVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MX[yN|k3PzF5Nx?=
MCF-7 FLV1000 MXrLbY5ie2ViQYPzZZk> NFHkOWsx6oDVM{CgxtVO MVO1JI1qdg>? MnfX[IVkemWjc3XzJHsyOjWLXT3JRWFRKHCqb4TvcIFj\Wyrbnegc4YhSUKFQkGgZZQhUUN3MDDv[kA{NjNizszN M{noSlI{QTZ5MUe3
MCF-7 FLV1000 M4LWPWtqdmG|ZTDBd5NigQ>? NVXST25lOOLCk{OwJOK2VQ>? MmXROUBucW5? M2LCVIRm[3KnYYPld{BcOTJ3SW2tTWFCWCCyaH;0c4xi[mWuaX7nJI9nKEGEQ1KyJIF1KEmFNUCgc4YhOC5yNzFOwG0> M3PLd|I{QTZ5MUe3
K562/ABCG2 NUXLOI1LS2WubDDWbYFjcWyrdImgRZN{[Xm| NYexUlFOOC5zL{CuOU8yKML3TR?= M3ix[Vk3KGh? MoLpd4Vve2m2aYrld{BMPTZ{L1HCR2czKGOnbHzzJJRwKG2rdH;4ZY51em:wZTD0c5BwfGWlYX9CpC=> MWqyN|k3PzF5Nx?=
8226/MR20 NXTCeYx3S2WubDDWbYFjcWyrdImgRZN{[Xm| MoS0NE4yKML3TR?= NGDWV286PiCq NWjjO5Jze2Wwc3n0bZpmeyCNNU[yM2FDS0d{IHPlcIx{KHSxIH3peI95[W62cn;u[UB1d3CxdHXjZY7DqA>? Mnf3NlM6PjdzN{e=
HMC1.1 MmrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fkVWlEPTB;MUSgcm0> NFTBNYwzOzR7N{OxOy=>
HMC1.2 NYPsRmhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrKeGlKSzVyPUG3Nlchdk1? M2PjR|I{PDl5M{G3
p815 MnrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\RSINNUUN3ME20OFUhdk1? NXzxeZNVOjN2OUezNVc>
Kasumi-1 NVXU[2d2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTN4IH7N M4jxd|I{PDl5M{G3
M-07e + SCF NH;POI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTd5IH7N Mn2zNlM1QTd|MUe=
EOL-1 NXmze5VXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETiNpVKSzVyPUGgcm0> M{L5cFI{PDl5M{G3
MV4;11 NITJTZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnIV2c5UUN3MEygNUBvVQ>? Ml7MNlM1QTd|MUe=
MOLM14 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrCTWpXUUN3MEygNUBvVQ>? M4PpN|I{PDl5M{G3
Pat.221 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fPTmlEPTB;Nke1JI5O MWmyN|Q6PzNzNx?=
Pat.279 M4m0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnSfXNvUUN3ME2zOFM1KG6P MWSyN|Q6PzNzNx?=
Pat.299 NUXjUYdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LBRmlEPTB;N{K0PEBvVQ>? M3vTWFI{PDl5M{G3
Pat.305 M2[xRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M365UWlEPTB;N{C3PUBvVQ>? NH74elkzOzR7N{OxOy=>
Pat.375 NF;RSmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT1NYF2UUN3ME21NFMhdk1? MYmyN|Q6PzNzNx?=
Pat.379 NHOzeVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRThyNjDuUS=> MX:yN|Q6PzNzNx?=
Pat.368 MmfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTJ5MECgcm0> MVOyN|Q6PzNzNx?=
Pat.601 MlzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3LUpR4UUN3ME2xNVU{KG6P NITHflYzOzR7N{OxOy=>
HMC1.1 NYSxR4VvSXCxcITvd4l{KEG|c3H5 MVfJR|UxRTNzIH7N MVGyN|Q6PzNzNx?=
p815 NUjSSGdzSXCxcITvd4l{KEG|c3H5 M2ryemlEPTB;M{SxJI5O M3\QXFI{PDl5M{G3
Kasumi-1 NFPhbGJCeG:ydH;zbZMhSXO|YYm= MmTSTWM2OD14NzDuUS=> NUHSW3p3OjN2OUezNVc>
M-07e + SCF MlrrRZBweHSxc3nzJGF{e2G7 NHjqXoxKSzVyPUe4JI5O M3rD[VI{PDl5M{G3
EOL-1 NFXNSVdCeG:ydH;zbZMhSXO|YYm= MVLJR|UxRCBzIH7N NUjLeJNoOjN2OUezNVc>
MV4;11 NIHI[|dCeG:ydH;zbZMhSXO|YYm= M2qw[GlEPTB;MjDuUS=> NEn0cXYzOzR7N{OxOy=>
MOLM14 Mo\ZRZBweHSxc3nzJGF{e2G7 NWnWW5diUUN3ME2zJI5O NWTnTGl5OjN2OUezNVc>
GIST822 Mnq1RZBweHSxc3nzJGF{e2G7 NWHWOYZNUUN3ME2xNFkhdk1? NXe4RVdNOjN2OUezNVc>
Pat.368 NGP4cmRCeG:ydH;zbZMhSXO|YYm= M1TxXmlEPTB;Mkm5PEBvVQ>? M4nmPFI{PDl5M{G3
Pat.601 NUXNRph2SXCxcITvd4l{KEG|c3H5 MXrJR|UxRTh5NjDuUS=> NFPlXIgzOzR7N{OxOy=>
MV4-11 M3LTRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\pb|czKGh? NFTKTIZKSzVyPUCuN{BvVQ>? Mke3NlM1OTJ7M{G=
MOLM-14 NEnHd5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DYVVczKGh? MoDsTWM2OD1yLkGgcm0> MUOyN|QyOjl|MR?=
SEM-K2 NXzFOnd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkP6O|IhcA>? MonZTWM2OD1yLkSgcm0> NUKxbFZ6OjN2MUK5N|E>
RS4;11 NIjWO|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXPO|IhcA>? MkTlTWM2OD5zMDywNFAhdk1? MmfrNlM1OTJ7M{G=
THP-1 NVXVeIdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrZOHBoPzJiaB?= M3XnfGlEPTB-MUCsNFAxKG6P Mk\hNlM1OTJ7M{G=
MV4-11 NVn0TVg4SXCxcITvd4l{KEG|c3H5 NXzWTYxVQC9{NDDo MXXpcoR2[2W|IIPp[45q\mmlYX70JIFv\CCmb4PlMYRmeGWwZHXueEBRSVKSIHPs[YF3[WenIHHu[EBi[2O3bYXsZZRqd25ib3[gd5VjNTKQIFTORS=> MoflNlM1OTJ7M{G=
MOLM-14 MWDBdI9xfG:|aYOgRZN{[Xl? M1TsdFgwOjRiaB?= NIDjd4NqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? MWeyN|QyOjl|MR?=
SEM-K2 Mlq0RZBweHSxc3nzJGF{e2G7 MnLiPE8zPCCq MV3pcoR2[2W|IIPp[45q\mmlYX70JIFv\CCmb4PlMYRmeGWwZHXueEBRSVKSIHPs[YF3[WenIHHu[EBi[2O3bYXsZZRqd25ib3[gd5VjNTKQIFTORS=> M4HPZ|I{PDF{OUOx
MV4-11 MonxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3GO|IhcA>? MUXJR|UxRTBwNU[gxtEhOC5|IH7N NIHkcWIyQTZ3NESwPC=>
A375 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYOyNG1XPzJiaB?= MV3JR|UxRiBzMDCwNFAhdk1? MVyxPVY2PDRyOB?=

... 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 individually and in order:
15% Captisol
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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID