Quizartinib (AC220)

製品コードS1526

Quizartinib (AC220)化学構造

分子量(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.

サイズ 価格(税別)  
In DMSO JPY 60500
JPY 36800
JPY 63400
JPY 163000
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バルク問合せ

文献中Selleckの製品使用例(36)

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) 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.
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 M{PZc2Z2dmO2aX;uJGF{e2G7 NWLBbZdvOC5zLUGwJO69VQ>? MkDKN|AhdWmw NULoNJJY\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ Ml:wNlM6PjdzN{e=
K562/ABCB1 MWjGeY5kfGmxbjDBd5NigQ>? Mkf4NE4yNTFyIN88US=> NXvKfFhSOzBibXnu NFfMflFmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MkTWNlM6PjdzN{e=
8226/MR20  NGjEfmpHfW6ldHnvckBCe3OjeR?= NUTHXZN[OC5zLUGwJO69VQ>? MVqzNEBucW5? NGPiPYhmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NXXkbG8yOjN7NkexO|c>
K562/ABCG2 NFL5SZdHfW6ldHnvckBCe3OjeR?= M1;YclAvOS1zMDFOwG0> MnHjN|AhdWmw MWjlcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MYWyN|k3PzF5Nx?=
MCF-7 FLV1000 M13lXGtqdmG|ZTDBd5NigQ>? NUOxbY12OOLCk{OwJOK2VQ>? MUS1JI1qdg>? NULmNItm\GWlcnXhd4V{KFtzMkXJYU1KSUGSIIDoc5RwdGGkZXzpcochd2ZiQVLDRlEh[XRiSVO1NEBw\iB|LkOg{txO MYmyN|k3PzF5Nx?=
MCF-7 FLV1000 NGC2OmNMcW6jc3WgRZN{[Xl? NEj2PIUx6oDVM{CgxtVO MXS1JI1qdg>? NUjtSVJJ\GWlcnXhd4V{KFtzMkXJYU1KSUGSIIDoc5RwdGGkZXzpcochd2ZiQVLDRlIh[XRiSVO1NEBw\iByLkC3JO69VQ>? NVewNJN[OjN7NkexO|c>
K562/ABCG2 M4n6[mNmdGxiVnnhZoltcXS7IFHzd4F6ew>? M2j0TFAvOS9yLkWvNUDDvU1? NYrqNpNxQTZiaB?= M4rZZpNmdnOrdHn6[ZMhUzV4Mj;BRmNIOiClZXzsd{B1dyCvaYTvfIFvfHKxbnWgeI9xd3SnY3HuxsA> M4\BVFI{QTZ5MUe3
8226/MR20 NFHJUlVE\WyuIG\pZYJqdGm2eTDBd5NigXN? Mli2NE4yKML3TR?= MYO5OkBp M2m4UZNmdnOrdHn6[ZMhUzV4Mj;BRmNIOiClZXzsd{B1dyCvaYTvfIFvfHKxbnWgeI9xd3SnY3HuxsA> Mn\qNlM6PjdzN{e=
HMC1.1 M4\y[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvtS4RKSzVyPUG0JI5O NWnwOIdNOjN2OUezNVc>
HMC1.2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHYPXlKSzVyPUG3Nlchdk1? NVn6XHZKOjN2OUezNVc>
p815 Ml70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPVOpZ5UUN3ME20OFUhdk1? M1:4[VI{PDl5M{G3
Kasumi-1 NUfPPGc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrrTWM2OD1|NjDuUS=> NWHCNJY1OjN2OUezNVc>
M-07e + SCF NFuxRmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTd5IH7N MkLuNlM1QTd|MUe=
EOL-1 M4\zcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITzZY5KSzVyPUGgcm0> NUfGbWhVOjN2OUezNVc>
MV4;11 NUPIe3lrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PqdmlEPTB:IEGgcm0> MYqyN|Q6PzNzNx?=
MOLM14 MmS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPuSmJKSzVyPDCxJI5O NFfwNHkzOzR7N{OxOy=>
Pat.221 M1LGPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorFTWM2OD14N{Wgcm0> NHrOS|IzOzR7N{OxOy=>
Pat.279 NHXhWHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTN2M{Sgcm0> MmjyNlM1QTd|MUe=
Pat.299 M3[3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nZU2lEPTB;N{K0PEBvVQ>? MX6yN|Q6PzNzNx?=
Pat.305 NWXHS5ZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;xWWlEPTB;N{C3PUBvVQ>? Ml3UNlM1QTd|MUe=
Pat.375 M4fGb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjBfmxtUUN3ME21NFMhdk1? NVX4Om9[OjN2OUezNVc>
Pat.379 Mn;IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkSyTWM2OD16ME[gcm0> MmHGNlM1QTd|MUe=
Pat.368 NWLpeGFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTJ5MECgcm0> NEXZUo4zOzR7N{OxOy=>
Pat.601 NGDVZY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFzNUOgcm0> MVuyN|Q6PzNzNx?=
HMC1.1 MXXBdI9xfG:|aYOgRZN{[Xl? NIfjeJBKSzVyPUOxJI5O MoL5NlM1QTd|MUe=
p815 NXzuRldFSXCxcITvd4l{KEG|c3H5 MVHJR|UxRTN2MTDuUS=> MkDyNlM1QTd|MUe=
Kasumi-1 NXmwcWNjSXCxcITvd4l{KEG|c3H5 M1qydGlEPTB;Nkegcm0> NH;JZnEzOzR7N{OxOy=>
M-07e + SCF Ml\nRZBweHSxc3nzJGF{e2G7 NEDhdFJKSzVyPUe4JI5O NIDIVWozOzR7N{OxOy=>
EOL-1 MljvRZBweHSxc3nzJGF{e2G7 MlHlTWM2ODxiMTDuUS=> MmT0NlM1QTd|MUe=
MV4;11 NYf5V|BzSXCxcITvd4l{KEG|c3H5 MnrGTWM2OD1{IH7N M{T3e|I{PDl5M{G3
MOLM14 M3XPSWFxd3C2b4Ppd{BCe3OjeR?= NXTM[m9oUUN3ME2zJI5O NFjVZoIzOzR7N{OxOy=>
GIST822 NWTaN21bSXCxcITvd4l{KEG|c3H5 MmfMTWM2OD1zMEmgcm0> MknnNlM1QTd|MUe=
Pat.368 MmHRRZBweHSxc3nzJGF{e2G7 NUTYeHpEUUN3ME2yPVk5KG6P M3rOXVI{PDl5M{G3
Pat.601 M1T5c2Fxd3C2b4Ppd{BCe3OjeR?= Mo\zTWM2OD16N{[gcm0> MnzaNlM1QTd|MUe=
MV4-11 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnKO|IhcA>? NInsS3RKSzVyPUCuN{BvVQ>? MVyyN|QyOjl|MR?=
MOLM-14 Mo\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nrblczKGh? NV31cZF3UUN3ME2wMlEhdk1? NXS1TGE3OjN2MUK5N|E>
SEM-K2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVe5VnBLPzJiaB?= M{jWbGlEPTB;MD60JI5O NYC4[4NHOjN2MUK5N|E>
RS4;11 NUjr[pNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\YRmw4OiCq MWXJR|UxRjFyLECwNEBvVQ>? MoHONlM1OTJ7M{G=
THP-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTaNGhuPzJiaB?= M4jpS2lEPTB-MUCsNFAxKG6P M1y1SVI{PDF{OUOx
MV4-11 MYLBdI9xfG:|aYOgRZN{[Xl? NEDROpQ5NzJ2IHi= NYfjUXYzcW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? NIS3cnUzOzRzMkmzNS=>
MOLM-14 MWrBdI9xfG:|aYOgRZN{[Xl? NGLkfY85NzJ2IHi= NHnMXVFqdmS3Y3XzJJNq\26rZnnjZY51KGGwZDDkc5NmNWSncHXu[IVvfCCSQWLQJINt\WG4YXflJIFv\CCjY3P1cZVt[XSrb36gc4Yhe3WkLULOJGRPSQ>? MkHXNlM1OTJ7M{G=
SEM-K2 NHnp[o9CeG:ydH;zbZMhSXO|YYm= MVS4M|I1KGh? M4LWUolv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C MkezNlM1OTJ7M{G=
MV4-11 MmPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXxNoZUPzJiaB?= MkOwTWM2OD1yLkW2JOKyKDBwMzDuUS=> NFnpXJAyQTZ3NESwPC=>
A375 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PvR|czKGh? M3H3RmlEPTB-IEGwJFAxOCCwTR?= MXGxPVY2PDRyOB?=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
p-STAT5 / STAT5 / β-catenin / p-AKT / AKT / p-ERK / ERK / p-S6 / S6; 

PubMed: 28625976     


Western blot analysis of AC220 treated MV4-11 cells. Cells were starved for overnight and treated with AC220 at indicated concentrations. Cells were harvested after 2 hours treatment and lysed. Then western blots analysis was performed. The quantification of bands are shown below the gel.

phospho-FLT3 / FLT3; 

PubMed: 22875611     


(B) The same cells were also harvested for Western blot analysis after treatment for 90 min with different concentrations of AC220. The phosphorylation of the different FLT3 proteins was determined using a phospho-FLT3 antibody.

28625976 22875611
Immunofluorescence
WGA / FLT3 ; 

PubMed: 28895560     


Immunofluorescence staining of FLT3-WT, FLT3 mutants or empty vector with or without AC220 treatment in transiently transfected U2OS cells. WGA (wheat germ agglutinin). Scale bar: 25 μm.

28895560
Growth inhibition assay
Cell viability; 

PubMed: 23967177     


K562/ABCB1 and K562/ABCG2 cells exhibit collateral sensitivity toquizartinib. K562, K562/ABCB1 and K562/ABCG2 cells were plated in the presence of quizartinib in increasing concentrations for 96 hours and viable cells were measured using the WST-1 assay.

23967177
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 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
15% Captisol
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程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

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    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

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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 ( 入力 出力 )

  • 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

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02984995 Completed Leukemia Myeloid Acute Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. December 2016 Phase 2
NCT02675478 Completed Relapsed AML|Refractory AML Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. February 2016 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    Is it possible to alter the captisol concentration to make it more dissolvable i.e 20% or 25% captisol ?

  • 回答:

    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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID