Quizartinib (AC220)

製品コードS1526

Quizartinib (AC220)化学構造

分子量(MW):560.67

Quizartinib (AC220)は一種の第二代FLT3阻害剤で、MV4-11と RS411細胞にFlt3(ITD/WT)に作用する時のIC50値が1.1 nM/4.2 nMです。Quizartinib (AC220)は、Flt3に作用する選択性はKIT、PDGFRA、PDGFRB、RETとCSF-1Rに作用する選択性より10倍が高くなります。臨床3期。

サイズ 価格 在庫  
JPY 50827.76 あり
JPY 30237.48 あり
JPY 53275.56 あり
JPY 139668.35 あり

カスタマーフィードバック(4)

  • 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.

製品安全説明書

FLT3阻害剤の選択性比較

生物活性

製品説明 Quizartinib (AC220)は一種の第二代FLT3阻害剤で、MV4-11と RS411細胞にFlt3(ITD/WT)に作用する時のIC50値が1.1 nM/4.2 nMです。Quizartinib (AC220)は、Flt3に作用する選択性はKIT、PDGFRA、PDGFRB、RETとCSF-1Rに作用する選択性より10倍が高くなります。臨床3期。
特性 The most potent cellular FLT3-ITD inhibitor.
ターゲット
FLT3 (ITD) [1]
(MV4-11 cells)
FLT3 (WT) [1]
(RS4;11 cells)
1.1 nM 4.2 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60/VCR NI\qZmxHfW6ldHnvckBCe3OjeR?= MWiwMlEuOTBizszN M3\USFMxKG2rbh?= MV\lcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NU\tRYJSOjN7NkexO|c>
K562/ABCB1 MWXGeY5kfGmxbjDBd5NigQ>? NFXPdWUxNjFvMUCg{txO MlG3N|AhdWmw Mlj5[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MkHNNlM6PjdzN{e=
8226/MR20  MmLuSpVv[3Srb36gRZN{[Xl? MYCwMlEuOTBizszN NFv2eJc{OCCvaX6= NIrIblNmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NHjTbJozOzl4N{G3Oy=>
K562/ABCG2 NY\RepNITnWwY4Tpc44hSXO|YYm= MkS1NE4yNTFyIN88US=> MVOzNEBucW5? M1\zdIVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MWqyN|k3PzF5Nx?=
MCF-7 FLV1000 MVjLbY5ie2ViQYPzZZk> MorHNQKBmzNyINM1US=> NYqxOpc2PSCvaX6= NV3MS3JK\GWlcnXhd4V{KFtzMkXJYU1KSUGSIIDoc5RwdGGkZXzpcochd2ZiQVLDRlEh[XRiSVO1NEBw\iB|LkOg{txO MkTnNlM6PjdzN{e=
MCF-7 FLV1000 MmHtT4lv[XOnIFHzd4F6 M2rnd|DjiJN|MDFCuW0> NFLybpA2KG2rbh?= MmXJ[IVkemWjc3XzJHsyOjWLXT3JRWFRKHCqb4TvcIFj\Wyrbnegc4YhSUKFQkKgZZQhUUN3MDDv[kAxNjB5IN88US=> M3[3XFI{QTZ5MUe3
K562/ABCG2 M{jJcWNmdGxiVnnhZoltcXS7IFHzd4F6ew>? MU[wMlEwOC53L{GgxtVO Mn\NPVYhcA>? NGrx[o5{\W6|aYTpfoV{KEt3NkKvRWJETzJiY3XscJMhfG9ibXn0c5hidnS{b37lJJRweG:2ZXPhcuKh NF:1cHgzOzl4N{G3Oy=>
8226/MR20 NY\yT4NrS2WubDDWbYFjcWyrdImgRZN{[Xm| NWDsZWlXOC5zINM1US=> M1e2TFk3KGh? MU\z[Y5{cXSrenXzJGs2PjJxQVLDS|Ih[2WubIOgeI8hdWm2b4jhcpRzd26nIITvdI91\WOjbtMg MmjoNlM6PjdzN{e=
HMC1.1 M3PMOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TLSGlEPTB;MUSgcm0> MXiyN|Q6PzNzNx?=
HMC1.2 NYnvdG1VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPUTWM2OD1zN{K3JI5O MX:yN|Q6PzNzNx?=
p815 NIXHWI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUf5cXlJUUN3ME20OFUhdk1? Mlr3NlM1QTd|MUe=
Kasumi-1 NH3CdY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGG0blNKSzVyPUO2JI5O M3zKR|I{PDl5M{G3
M-07e + SCF NGTLdnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rrS2lEPTB;N{egcm0> NED5dZMzOzR7N{OxOy=>
EOL-1 M2LuUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;nSGRGUUN3ME2xJI5O MoLQNlM1QTd|MUe=
MV4;11 NVXrcmFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITDclJKSzVyPDCxJI5O MX6yN|Q6PzNzNx?=
MOLM14 M2HKR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jjSGlEPTB:IEGgcm0> NH[3ZoszOzR7N{OxOy=>
Pat.221 MmP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEC3fW9KSzVyPU[3OUBvVQ>? MlzYNlM1QTd|MUe=
Pat.279 NH;Dbm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzPTWM2OD1|NEO0JI5O NXL1c|JHOjN2OUezNVc>
Pat.299 NU[zSJI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLvSoZJUUN3ME23NlQ5KG6P M3W3N|I{PDl5M{G3
Pat.305 NHfGN29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjETWM2OD15MEe5JI5O NUPJfXVSOjN2OUezNVc>
Pat.375 MoToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvJTWM2OD13MEOgcm0> NHu3SVEzOzR7N{OxOy=>
Pat.379 M2rhV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnF[FlKSzVyPUiwOkBvVQ>? NIex[lUzOzR7N{OxOy=>
Pat.368 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmOxTWM2OD1{N{CwJI5O M1TRTVI{PDl5M{G3
Pat.601 M2HHNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\CcGlEPTB;MUG1N{BvVQ>? NVjYcGR[OjN2OUezNVc>
HMC1.1 MVLBdI9xfG:|aYOgRZN{[Xl? M1\JeWlEPTB;M{Ggcm0> MXKyN|Q6PzNzNx?=
p815 MkCyRZBweHSxc3nzJGF{e2G7 NUP6eIh3UUN3ME2zOFEhdk1? M2jpTlI{PDl5M{G3
Kasumi-1 MXjBdI9xfG:|aYOgRZN{[Xl? MlHiTWM2OD14NzDuUS=> MlTINlM1QTd|MUe=
M-07e + SCF MVjBdI9xfG:|aYOgRZN{[Xl? MlrOTWM2OD15ODDuUS=> M2POW|I{PDl5M{G3
EOL-1 MUPBdI9xfG:|aYOgRZN{[Xl? NYHre|h[UUN3MEygNUBvVQ>? Mli4NlM1QTd|MUe=
MV4;11 NWDnPGs6SXCxcITvd4l{KEG|c3H5 Mk\2TWM2OD1{IH7N NIjsS4QzOzR7N{OxOy=>
MOLM14 NXSzTZFLSXCxcITvd4l{KEG|c3H5 NW\ZXmMyUUN3ME2zJI5O MUWyN|Q6PzNzNx?=
GIST822 MWLBdI9xfG:|aYOgRZN{[Xl? NHf2VGdKSzVyPUGwPUBvVQ>? M2L0UVI{PDl5M{G3
Pat.368 NEjLT|BCeG:ydH;zbZMhSXO|YYm= M1TOVWlEPTB;Mkm5PEBvVQ>? MoCyNlM1QTd|MUe=
Pat.601 NETRUotCeG:ydH;zbZMhSXO|YYm= NGrT[2lKSzVyPUi3OkBvVQ>? M2H0T|I{PDl5M{G3
MV4-11 NVK2SGRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jqd|czKGh? NYrP[mlCUUN3ME2wMlMhdk1? Mni3NlM1OTJ7M{G=
MOLM-14 NH62RXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjZbo1KPzJiaB?= NGjUO3ZKSzVyPUCuNUBvVQ>? Ml3jNlM1OTJ7M{G=
SEM-K2 M{jDSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLEblhSPzJiaB?= MnjBTWM2OD1yLkSgcm0> M{XIb|I{PDF{OUOx
RS4;11 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVy3NkBp NU\kVoFPUUN3ME6xNEwxODBibl2= MUWyN|QyOjl|MR?=
THP-1 NHPicFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlizO|IhcA>? M2HycGlEPTB-MUCsNFAxKG6P MoqxNlM1OTJ7M{G=
MV4-11 NEDJPYhCeG:ydH;zbZMhSXO|YYm= NGnSW5U5NzJ2IHi= M17YWolv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C NHfZdJIzOzRzMkmzNS=>
MOLM-14 MVjBdI9xfG:|aYOgRZN{[Xl? MUC4M|I1KGh? NH7vRpdqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? NEjVfYUzOzRzMkmzNS=>
SEM-K2 MWPBdI9xfG:|aYOgRZN{[Xl? MYe4M|I1KGh? NHLXSmZqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? NIG1OmozOzRzMkmzNS=>
MV4-11 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1f1ZVczKGh? MmHhTWM2OD1yLkW2JOKyKDBwMzDuUS=> M4HDW|E6PjV2NEC4
A375 M4jTdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfMO|IhcA>? M1PlWWlEPTB-IEGwJFAxOCCwTR?= MXWxPVY2PDRyOB?=

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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
細胞試験: [1]
+ 展開
  • 細胞株: MV4-11 and RS4;11 cells
  • 濃度: Dissolved in DMSO, final concentration ~20 μM
  • 反応時間: 72 hours
  • 実験の流れ: 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
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: Female NU/NU or severe combined immunodeficient mice implanted with MV4-11 cells
  • 製剤: Formulated in 22% hydroxypropyl-β-cyclodextrin
  • 投薬量: ~10 mg/kg
  • 投与方法: Oral gavage
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 33 mg/mL (58.85 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
15% Captisol
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 560.67
化学式

C29H32N6O4S

CAS No. 950769-58-1
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

FLT3信号経路図

FLT3 Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID