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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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 MknQSpVv[3Srb36gRZN{[Xl? MlO4NE4yNTFyIN88US=> MlnGN|AhdWmw Mlnq[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NUPkb3k5OjN7NkexO|c>
K562/ABCB1 NHfMSHJHfW6ldHnvckBCe3OjeR?= MUiwMlEuOTBizszN NYjOVpNJOzBibXnu M{jNb4VvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NX3TOnJLOjN7NkexO|c>
8226/MR20  NVfFbVFLTnWwY4Tpc44hSXO|YYm= M{X5NlAvOS1zMDFOwG0> MYGzNEBucW5? M3PHeYVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? Mn;XNlM6PjdzN{e=
K562/ABCG2 M2fZS2Z2dmO2aX;uJGF{e2G7 NInDcI8xNjFvMUCg{txO NXfBZZhiOzBibXnu MnTI[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NE\BOWwzOzl4N{G3Oy=>
MCF-7 FLV1000 NGTqcXJMcW6jc3WgRZN{[Xl? NH7PW3Mx6oDVM{CgxtVO NWK5bWxXPSCvaX6= NFjZd2tl\WO{ZXHz[ZMhYzF{NVndMWlCSVBicHjveI9t[WKnbHnu[{Bw\iCDQlPCNUBifCCLQ{WwJI9nKDNwMzFOwG0> NFu3UFIzOzl4N{G3Oy=>
MCF-7 FLV1000 MoX3T4lv[XOnIFHzd4F6 NUjYTW92OOLCk{OwJOK2VQ>? M3XRZlUhdWmw NULrZXBT\GWlcnXhd4V{KFtzMkXJYU1KSUGSIIDoc5RwdGGkZXzpcochd2ZiQVLDRlIh[XRiSVO1NEBw\iByLkC3JO69VQ>? MXSyN|k3PzF5Nx?=
K562/ABCG2 M3vTUWNmdGxiVnnhZoltcXS7IFHzd4F6ew>? Ml3RNE4yNzBwNT:xJOK2VQ>? M4Swdlk3KGh? MV;z[Y5{cXSrenXzJGs2PjJxQVLDS|Ih[2WubIOgeI8hdWm2b4jhcpRzd26nIITvdI91\WOjbtMg NEPMPWszOzl4N{G3Oy=>
8226/MR20 NVSybmxxS2WubDDWbYFjcWyrdImgRZN{[Xm| M2PWXFAvOSEEtV2= NWrvNVFEQTZiaB?= NGLq[4J{\W6|aYTpfoV{KEt3NkKvRWJETzJiY3XscJMhfG9ibXn0c5hidnS{b37lJJRweG:2ZXPhcuKh Mn6yNlM6PjdzN{e=
HMC1.1 M3HkXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTkTIxKSzVyPUG0JI5O MUWyN|Q6PzNzNx?=
HMC1.2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTCTWM2OD1zN{K3JI5O NGe1dIszOzR7N{OxOy=>
p815 NIm4b2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPtTWM2OD12NEWgcm0> MnzpNlM1QTd|MUe=
Kasumi-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTN4IH7N MkXvNlM1QTd|MUe=
M-07e + SCF NXfXVmRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIn1VlhKSzVyPUe3JI5O MYOyN|Q6PzNzNx?=
EOL-1 NXXDU2lST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrsb5p4UUN3ME2xJI5O MmW0NlM1QTd|MUe=
MV4;11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmD2TWM2ODxiMTDuUS=> NF3jWWUzOzR7N{OxOy=>
MOLM14 M2mzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRCBzIH7N NXe1ZmdOOjN2OUezNVc>
Pat.221 MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vWdWlEPTB;Nke1JI5O MkTwNlM1QTd|MUe=
Pat.279 Moi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTN2M{Sgcm0> NXXrOlBuOjN2OUezNVc>
Pat.299 MlzXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTd{NEigcm0> MXyyN|Q6PzNzNx?=
Pat.305 Mn3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD4Z|FlUUN3ME23NFc6KG6P M{nwZlI{PDl5M{G3
Pat.375 MmLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTVyMzDuUS=> NEfmRnQzOzR7N{OxOy=>
Pat.379 NULLPWFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGS1cHRKSzVyPUiwOkBvVQ>? MV6yN|Q6PzNzNx?=
Pat.368 NEn0[|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3j4dmlEPTB;MkewNEBvVQ>? MoizNlM1QTd|MUe=
Pat.601 MoTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL1Vo0zUUN3ME2xNVU{KG6P MUSyN|Q6PzNzNx?=
HMC1.1 NHT6PJVCeG:ydH;zbZMhSXO|YYm= NXH2[41TUUN3ME2zNUBvVQ>? NHLBXmUzOzR7N{OxOy=>
p815 MXLBdI9xfG:|aYOgRZN{[Xl? NYWycnM3UUN3ME2zOFEhdk1? MnfLNlM1QTd|MUe=
Kasumi-1 MmDJRZBweHSxc3nzJGF{e2G7 NYSzR285UUN3ME22O{BvVQ>? MkTaNlM1QTd|MUe=
M-07e + SCF MnvDRZBweHSxc3nzJGF{e2G7 NUTHUW1qUUN3ME23PEBvVQ>? NYS0U49bOjN2OUezNVc>
EOL-1 MlvBRZBweHSxc3nzJGF{e2G7 M2roN2lEPTB:IEGgcm0> MVeyN|Q6PzNzNx?=
MV4;11 NWrScWV1SXCxcITvd4l{KEG|c3H5 Mlv5TWM2OD1{IH7N MWOyN|Q6PzNzNx?=
MOLM14 MnrZRZBweHSxc3nzJGF{e2G7 MX3JR|UxRTNibl2= MmDjNlM1QTd|MUe=
GIST822 MVTBdI9xfG:|aYOgRZN{[Xl? MXjJR|UxRTFyOTDuUS=> Ml72NlM1QTd|MUe=
Pat.368 M4Gz[GFxd3C2b4Ppd{BCe3OjeR?= MkPuTWM2OD1{OUm4JI5O NXPySVl{OjN2OUezNVc>
Pat.601 M3PteGFxd3C2b4Ppd{BCe3OjeR?= MlG5TWM2OD16N{[gcm0> NXnpZ5pLOjN2OUezNVc>
MV4-11 NEjVcolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TyVFczKGh? M3G0SWlEPTB;MD6zJI5O NWnRTZFjOjN2MUK5N|E>
MOLM-14 Mnv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWW3NkBp MomzTWM2OD1yLkGgcm0> MXGyN|QyOjl|MR?=
SEM-K2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVy3NkBp M2LQZ2lEPTB;MD60JI5O NGPMWY8zOzRzMkmzNS=>
RS4;11 M13R[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXCbGk4OiCq MXfJR|UxRjFyLECwNEBvVQ>? MWiyN|QyOjl|MR?=
THP-1 MnHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmKzO|IhcA>? NWPPNI1iUUN3ME6xNEwxODBibl2= NH\pSGkzOzRzMkmzNS=>
MV4-11 M3OwbmFxd3C2b4Ppd{BCe3OjeR?= MVO4M|I1KGh? M{f0UIlv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C MlvkNlM1OTJ7M{G=
MOLM-14 NEHRXo9CeG:ydH;zbZMhSXO|YYm= NYL6SnRRQC9{NDDo MUnpcoR2[2W|IIPp[45q\mmlYX70JIFv\CCmb4PlMYRmeGWwZHXueEBRSVKSIHPs[YF3[WenIHHu[EBi[2O3bYXsZZRqd25ib3[gd5VjNTKQIFTORS=> NVzBTWx1OjN2MUK5N|E>
SEM-K2 MV3BdI9xfG:|aYOgRZN{[Xl? MXG4M|I1KGh? NFvTZ4xqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? NYLQZXl2OjN2MUK5N|E>
MV4-11 NYOzWG9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nNUVczKGh? M3[5[2lEPTB;MD61OkDDuSByLkOgcm0> NVP3S|VTOTl4NUS0NFg>
A375 NWPpSodQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDWS4g4OiCq MYrJR|UxRiBzMDCwNFAhdk1? Mli5NVk3PTR2MEi=

... 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 33.2 mg/mL (59.21 mM)
Water <0.3 mg/mL
Ethanol <0.5 mg/mL
In vivo 15% Captisol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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