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(税別)  
JPY 58598.00
JPY 34860.00
JPY 61420.00
JPY 161020.00

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 Mk[3SpVv[3Srb36gRZN{[Xl? MY[wMlEuOTBizszN MnTPN|AhdWmw NF3xUHFmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NIDlO4EzOzl4N{G3Oy=>
K562/ABCB1 NF65SWRHfW6ldHnvckBCe3OjeR?= MWmwMlEuOTBizszN NIXhPZE{OCCvaX6= M1vE[YVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NWHwcHNDOjN7NkexO|c>
8226/MR20  NWrCenF1TnWwY4Tpc44hSXO|YYm= NGO1UpgxNjFvMUCg{txO Mni3N|AhdWmw NWjNVnEx\W6qYX7j[ZMhfXC2YXvlJI9nKHO3YoP0doF1\XNib3[gRWJETzJiYX7kJGFDS0JzIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MXGyN|k3PzF5Nx?=
K562/ABCG2 MoTZSpVv[3Srb36gRZN{[Xl? MV2wMlEuOTBizszN M2DoNVMxKG2rbh?= MUflcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MV:yN|k3PzF5Nx?=
MCF-7 FLV1000 Mnj6T4lv[XOnIFHzd4F6 NEXMZXgx6oDVM{CgxtVO MYm1JI1qdg>? MVfk[YNz\WG|ZYOgX|EzPUmfLVnBRXAheGixdH;sZYJmdGmwZzDv[kBCSkOEMTDheEBKSzVyIH;mJFMvOyEQvF2= M3vvOVI{QTZ5MUe3
MCF-7 FLV1000 MmLDT4lv[XOnIFHzd4F6 MWSw5qCUOzBiwsXN NFLodHM2KG2rbh?= MmG1[IVkemWjc3XzJHsyOjWLXT3JRWFRKHCqb4TvcIFj\Wyrbnegc4YhSUKFQkKgZZQhUUN3MDDv[kAxNjB5IN88US=> M3mwclI{QTZ5MUe3
K562/ABCG2 M4m1b2NmdGxiVnnhZoltcXS7IFHzd4F6ew>? Mk\mNE4yNzBwNT:xJOK2VQ>? M3TLb|k3KGh? M1nKcJNmdnOrdHn6[ZMhUzV4Mj;BRmNIOiClZXzsd{B1dyCvaYTvfIFvfHKxbnWgeI9xd3SnY3HuxsA> NWjSS3NiOjN7NkexO|c>
8226/MR20 NVPDbHVES2WubDDWbYFjcWyrdImgRZN{[Xm| MUKwMlEhyrWP MYe5OkBp NU\GdnQze2Wwc3n0bZpmeyCNNU[yM2FDS0d{IHPlcIx{KHSxIH3peI95[W62cn;u[UB1d3CxdHXjZY7DqA>? M{XxblI{QTZ5MUe3
HMC1.1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\GUGlEPTB;MUSgcm0> Mmn2NlM1QTd|MUe=
HMC1.2 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rtUWlEPTB;MUeyO{BvVQ>? MkPYNlM1QTd|MUe=
p815 Mkf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHhTWM2OD12NEWgcm0> M3fLbFI{PDl5M{G3
Kasumi-1 M3m2NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnnTWM2OD1|NjDuUS=> NH7zfWozOzR7N{OxOy=>
M-07e + SCF NXvle4Z5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTd5IH7N M2nqeVI{PDl5M{G3
EOL-1 M3fhZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHCTWM2OD1zIH7N M4LJRVI{PDl5M{G3
MV4;11 NXH3bIVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\ZTWM2ODxiMTDuUS=> NVrrNoFHOjN2OUezNVc>
MOLM14 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRCBzIH7N M1y3RlI{PDl5M{G3
Pat.221 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\zTWM2OD14N{Wgcm0> NFzXR4EzOzR7N{OxOy=>
Pat.279 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTN2M{Sgcm0> MXiyN|Q6PzNzNx?=
Pat.299 NFy4em1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTd{NEigcm0> MlyyNlM1QTd|MUe=
Pat.305 NEf1WGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\HUoxKSzVyPUewO|khdk1? MUKyN|Q6PzNzNx?=
Pat.375 M4Xsd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHRTWM2OD13MEOgcm0> MVWyN|Q6PzNzNx?=
Pat.379 M3Lxcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIX2bG5KSzVyPUiwOkBvVQ>? MoXENlM1QTd|MUe=
Pat.368 M{\4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zmOWlEPTB;MkewNEBvVQ>? M{CzXlI{PDl5M{G3
Pat.601 MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XJb2lEPTB;MUG1N{BvVQ>? NYTxOZduOjN2OUezNVc>
HMC1.1 M4jxNWFxd3C2b4Ppd{BCe3OjeR?= NEPSfVZKSzVyPUOxJI5O NGPyRngzOzR7N{OxOy=>
p815 MX;BdI9xfG:|aYOgRZN{[Xl? Ml3CTWM2OD1|NEGgcm0> MV6yN|Q6PzNzNx?=
Kasumi-1 NIrpbXRCeG:ydH;zbZMhSXO|YYm= NEH6Z5BKSzVyPU[3JI5O MmS4NlM1QTd|MUe=
M-07e + SCF NEPCdWZCeG:ydH;zbZMhSXO|YYm= NYLDTnJ5UUN3ME23PEBvVQ>? MU[yN|Q6PzNzNx?=
EOL-1 MX;BdI9xfG:|aYOgRZN{[Xl? Mn\BTWM2ODxiMTDuUS=> M1m4cFI{PDl5M{G3
MV4;11 MmfXRZBweHSxc3nzJGF{e2G7 NYOwfJZtUUN3ME2yJI5O M{XVXlI{PDl5M{G3
MOLM14 NUOyeWtMSXCxcITvd4l{KEG|c3H5 MWXJR|UxRTNibl2= MkG0NlM1QTd|MUe=
GIST822 NVrESZJUSXCxcITvd4l{KEG|c3H5 MW\JR|UxRTFyOTDuUS=> NFXkbZczOzR7N{OxOy=>
Pat.368 MXHBdI9xfG:|aYOgRZN{[Xl? MmX0TWM2OD1{OUm4JI5O M{nYTVI{PDl5M{G3
Pat.601 NF\JOIVCeG:ydH;zbZMhSXO|YYm= NGn1NFZKSzVyPUi3OkBvVQ>? M{X0cVI{PDl5M{G3
MV4-11 M4XueWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[5O|IhcA>? NULCeIxKUUN3ME2wMlMhdk1? M1HvSVI{PDF{OUOx
MOLM-14 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTqWG03PzJiaB?= NFLV[5lKSzVyPUCuNUBvVQ>? MorqNlM1OTJ7M{G=
SEM-K2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXzOYs4OiCq NHPucGFKSzVyPUCuOEBvVQ>? Mk\mNlM1OTJ7M{G=
RS4;11 M1qwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LpeFczKGh? Mom1TWM2OD5zMDywNFAhdk1? MXqyN|QyOjl|MR?=
THP-1 NEnLc49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnv6O|IhcA>? MYfJR|UxRjFyLECwNEBvVQ>? MmX6NlM1OTJ7M{G=
MV4-11 MVPBdI9xfG:|aYOgRZN{[Xl? NV31RpZWQC9{NDDo NVLKZYJxcW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? NWnZ[lRUOjN2MUK5N|E>
MOLM-14 NVTTd41YSXCxcITvd4l{KEG|c3H5 M{XMdFgwOjRiaB?= Mmr0bY5lfWOnczDzbYdvcW[rY3HueEBidmRiZH;z[U1l\XCnbnTlcpQhWEGUUDDjcIVifmGpZTDhcoQh[WOldX31cIF1cW:wIH;mJJN2[i1{TjDEUmE> NGTxbYYzOzRzMkmzNS=>
SEM-K2 NGj4eW1CeG:ydH;zbZMhSXO|YYm= MYm4M|I1KGh? Ml;HbY5lfWOnczDzbYdvcW[rY3HueEBidmRiZH;z[U1l\XCnbnTlcpQhWEGUUDDjcIVifmGpZTDhcoQh[WOldX31cIF1cW:wIH;mJJN2[i1{TjDEUmE> NFi4T2czOzRzMkmzNS=>
MV4-11 NIPncZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LXPFczKGh? M{HmS2lEPTB;MD61OkDDuSByLkOgcm0> MV[xPVY2PDRyOB?=
A375 M{\VS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWe3NkBp NUXCcYFIUUN3ME6gNVAhODByIH7N NXTzS5ZOOTl4NUS0NFg>

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
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

よくある質問(FAQ)

  • 問題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