Quizartinib (AC220)

目录号:S1526 中文名称:奎扎替尼

仅限科研使用

Quizartinib (AC220)是一种二代FLT3抑制剂,作用于Flt3(ITD/WT),在MV4-11和 RS4;11细胞中IC50分别为1.1 nM/4.2 nM,作用于Flt3比作用于KIT,PDGFRA,PDGFRB,RET,和CSF-1R选择性高10倍。Quizartinib (AC220)可诱导肿瘤细胞的凋亡。Phase 3。

Quizartinib (AC220) Chemical Structure

CAS: 950769-58-1

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2891.02 现货
RMB 1729.76 现货
RMB 7933.51 现货
大包装 有超大折扣
大剂量询单有大折扣!

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
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客户使用Selleck生产的Quizartinib (AC220)发表文献114篇:

产品安全说明书

Target Protein Ligand抑制剂选择性比较

生物活性

产品描述 Quizartinib (AC220)是一种二代FLT3抑制剂,作用于Flt3(ITD/WT),在MV4-11和 RS4;11细胞中IC50分别为1.1 nM/4.2 nM,作用于Flt3比作用于KIT,PDGFRA,PDGFRB,RET,和CSF-1R选择性高10倍。Quizartinib (AC220)可诱导肿瘤细胞的凋亡。Phase 3。
特性 AC220是二代FLT3抑制剂,且作为临床FLT3抑制剂的第一候选药。
靶点
FLT3 (ITD) [1]
(MV4-11 cells)
FLT3 (WT) [1]
(RS4;11 cells)
1.1 nM 4.2 nM
体外研究

AC220是最有效的FLT3选择性抑制剂,可用于治疗急性骨髓性白血病(AML)。AC220在生化和细胞实验中具有低纳摩尔效果和特别的激酶选择性,抑制大部分人类蛋白激酶时具有高选择性。AC220是治疗急性骨髓性白血病(AML)的新型FLT3抑制剂。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60/VCR MkXQSpVv[3Srb36gRZN{[Xl? MV6wMlEuOTBizszN NUXCTY5KOzBibXnu M1rPboVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4N{G3O{c,OjN7NkexO|c9N2F-
K562/ABCB1 MnzFSpVv[3Srb36gRZN{[Xl? NU[zRmI5OC5zLUGwJO69VQ>? NHvyZmQ{OCCvaX6= M4jEW4VvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? M33vOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[3NVc4Lz5{M{m2O|E4PzxxYU6=
8226/MR20  NWHxVVdNTnWwY4Tpc44hSXO|YYm= NGe2Ro0xNjFvMUCg{txO NYLzc3Q5OzBibXnu M3vNUoVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NFTLPG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2O|E4Pyd-MkO5OlcyPzd:L3G+
K562/ABCG2 M33KTWZ2dmO2aX;uJGF{e2G7 M{DVbFAvOS1zMDFOwG0> NFfUV|A{OCCvaX6= NH:4elNmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NXXydVBbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlcyPzdpPkKzPVY4OTd5PD;hQi=>
MCF-7 FLV1000 NIPIb|lMcW6jc3WgRZN{[Xl? M{\Td|DjiJN|MDFCuW0> MkLTOUBucW5? NFT2U4pl\WO{ZXHz[ZMhYzF{NVndMWlCSVBicHjveI9t[WKnbHnu[{Bw\iCDQlPCNUBifCCLQ{WwJI9nKDNwMzFOwG0> M36zUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[3NVc4Lz5{M{m2O|E4PzxxYU6=
MCF-7 FLV1000 MnH1T4lv[XOnIFHzd4F6 M2CzNVDjiJN|MDFCuW0> MVW1JI1qdg>? NWH4dIFR\GWlcnXhd4V{KFtzMkXJYU1KSUGSIIDoc5RwdGGkZXzpcochd2ZiQVLDRlIh[XRiSVO1NEBw\iByLkC3JO69VQ>? NW\yZpF6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlcyPzdpPkKzPVY4OTd5PD;hQi=>
K562/ABCG2 NULL[nNwS2WubDDWbYFjcWyrdImgRZN{[Xm| MkD4NE4yNzBwNT:xJOK2VQ>? MmG0PVYhcA>? NE[w[pd{\W6|aYTpfoV{KEt3NkKvRWJETzJiY3XscJMhfG9ibXn0c5hidnS{b37lJJRweG:2ZXPhcuKh M2PUOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[3NVc4Lz5{M{m2O|E4PzxxYU6=
8226/MR20 M2LTS2NmdGxiVnnhZoltcXS7IFHzd4F6ew>? MlHDNE4yKML3TR?= NH;Zd3o6PiCq MkTad4Vve2m2aYrld{BMPTZ{L1HCR2czKGOnbHzzJJRwKG2rdH;4ZY51em:wZTD0c5BwfGWlYX9CpC=> M3OwNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[3NVc4Lz5{M{m2O|E4PzxxYU6=
HMC1.1 MnzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\GTWM2OD1zNDDuUS=> M2WydlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEm3N|E4Lz5{M{S5O|MyPzxxYU6=
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Pat.221 NH70OFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXXTWM2OD14N{Wgcm0> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR7N{OxO{c,OjN2OUezNVc9N2F-
Pat.279 M4PPVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnSTWM2OD1|NEO0JI5O MoDDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OUezNVcoRjJ|NEm3N|E4RC:jPh?=
Pat.299 M4\jWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonUTWM2OD15MkS4JI5O MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR7N{OxO{c,OjN2OUezNVc9N2F-
Pat.305 M33jWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTdyN{mgcm0> M{PNZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEm3N|E4Lz5{M{S5O|MyPzxxYU6=
Pat.375 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfFNHV6UUN3ME21NFMhdk1? NWrQb3E{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PVc{OTdpPkKzOFk4OzF5PD;hQi=>
Pat.379 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRThyNjDuUS=> MonFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OUezNVcoRjJ|NEm3N|E4RC:jPh?=
Pat.368 M2j0dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnKdJZKSzVyPUK3NFAhdk1? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR7N{OxO{c,OjN2OUezNVc9N2F-
Pat.601 M13rVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFzNUOgcm0> M2XVVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEm3N|E4Lz5{M{S5O|MyPzxxYU6=
HMC1.1 M33UWGFxd3C2b4Ppd{BCe3OjeR?= MkLITWM2OD1|MTDuUS=> NYO1cHhKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PVc{OTdpPkKzOFk4OzF5PD;hQi=>
p815 NEPvN4RCeG:ydH;zbZMhSXO|YYm= NUfQVnlLUUN3ME2zOFEhdk1? M{PoPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEm3N|E4Lz5{M{S5O|MyPzxxYU6=
Kasumi-1 MljPRZBweHSxc3nzJGF{e2G7 M2T6emlEPTB;Nkegcm0> MkfRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OUezNVcoRjJ|NEm3N|E4RC:jPh?=
M-07e + SCF NV7ZeoxYSXCxcITvd4l{KEG|c3H5 MWrJR|UxRTd6IH7N NIWwd5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S5O|MyPyd-MkO0PVc{OTd:L3G+
EOL-1 MnXrRZBweHSxc3nzJGF{e2G7 MorDTWM2ODxiMTDuUS=> NVmzVXZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PVc{OTdpPkKzOFk4OzF5PD;hQi=>
MV4;11 M{XnfmFxd3C2b4Ppd{BCe3OjeR?= MlP4TWM2OD1{IH7N NXv2U4JqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PVc{OTdpPkKzOFk4OzF5PD;hQi=>
MOLM14 MUjBdI9xfG:|aYOgRZN{[Xl? Ml\LTWM2OD1|IH7N MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR7N{OxO{c,OjN2OUezNVc9N2F-
GIST822 NHG5ZpVCeG:ydH;zbZMhSXO|YYm= NUWwNZNjUUN3ME2xNFkhdk1? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR7N{OxO{c,OjN2OUezNVc9N2F-
Pat.368 NHzXVlRCeG:ydH;zbZMhSXO|YYm= MVnJR|UxRTJ7OUigcm0> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR7N{OxO{c,OjN2OUezNVc9N2F-
Pat.601 NHnUTJVCeG:ydH;zbZMhSXO|YYm= MoDnTWM2OD16N{[gcm0> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR7N{OxO{c,OjN2OUezNVc9N2F-
MV4-11 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVi5[XFyPzJiaB?= MWrJR|UxRTBwMzDuUS=> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzRzMkmzNUc,OjN2MUK5N|E9N2F-
MOLM-14 MlnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUm3NkBp M2npSGlEPTB;MD6xJI5O M1jjWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEGyPVMyLz5{M{SxNlk{OTxxYU6=
SEM-K2 Mn\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn[1O|IhcA>? M1HJO2lEPTB;MD60JI5O NI\aRnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{SxNlk{OSd-MkO0NVI6OzF:L3G+
RS4;11 MnXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TBZlczKGh? MYnJR|UxRjFyLECwNEBvVQ>? M2XsTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEGyPVMyLz5{M{SxNlk{OTxxYU6=
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SEM-K2 M{XtRWFxd3C2b4Ppd{BCe3OjeR?= NF\RfXM5NzJ2IHi= MnfKbY5lfWOnczDzbYdvcW[rY3HueEBidmRiZH;z[U1l\XCnbnTlcpQhWEGUUDDjcIVifmGpZTDhcoQh[WOldX31cIF1cW:wIH;mJJN2[i1{TjDEUmE> NIm3U5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{SxNlk{OSd-MkO0NVI6OzF:L3G+
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Assay
Methods Test Index PMID
Western blot p-STAT5 / STAT5 / β-catenin / p-AKT / AKT / p-ERK / ERK / p-S6 / S6 phospho-FLT3 / FLT3 28625976 22875611
Immunofluorescence WGA / FLT3 28895560
Growth inhibition assay Cell viability 23967177
体内研究 AC220作用于移植瘤模型,具有好的药品属性,极高的药效和耐受性。在体内,AC220作用于FLT3-ITD AML鼠模型,抑制FLT3活性,明显延长寿命;作用于依赖FLT3的移植瘤鼠模型时,根除肿瘤;作用于病人原代细胞时,有效抑制FLT3活性。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
  • 激酶实验:

    为了测定AC220抑制无靶点激酶的效果,为了比较AC220和其他FLT抑制剂的选择性,使AC220作用于KinomeScan一组402种激酶进行结合试验,其中80%为典型的人类蛋白激酶。测定所有激酶的解离常数。计算绝对选择性和作用于FLT的相对选择性。

细胞实验:[1]
  • Cell lines: MV4-11和RS4;11细胞
  • Concentrations: 0-100 nM
  • Incubation Time: 72小时,及2小时
  • Method: 在增殖实验中,细胞培养在低血清培养基(含0.5% FBS)中过夜, 然后按每孔4×104个细胞接种在96孔板上,然后加入AC220,37oC下温育72小时。测定细胞活力。测定抑制FLT3自磷酸化的效果, 细胞培养在低血清培养基(含0.5% FBS)过夜,然后按每孔4×105个细胞接种在96孔板上。细胞和AC220一起在37oC下温育2小时,诱导 RS4;11细胞中FLT3自磷酸化, 加入100 ng/mL FLT3配位体,持续15分钟。转移细胞溶解物到用FLT3抗体包被的96孔板上。然后加入作用于FLT3的生物素化抗体,测定全部FLT3,或者作用于磷酸酪氨酸的抗体,测定FLT3自磷酸化。使用 SULFO标记的链霉亲和素二抗进行电化学发光测定。
动物实验:[1]
  • Animal Models: 雌性裸鼠或严重联合免疫缺陷鼠
  • Dosages: 10 mL/kg
  • Administration: 口服饲喂处理

溶解度(25°C)

体外

体内

从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
15% Captisol

30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 560.67
化学式

C29H32N6O4S

CAS号 950769-58-1
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04459598 Completed Drug: Efavirenz|Drug: Quizartinib Healthy Subjects|Drug-drug Interaction|Pharmacokinetics|Quizartinib Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. September 8 2020 Early Phase 1
NCT04473664 Completed Drug: Quizartinib Hepatic Impairment|Moderate Impaired Hepatic Function Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. September 29 2020 Phase 1
NCT04459585 Completed Drug: Dabigatran Etexilate Mesylate|Drug: Quizartinib Healthy Subjects|Drug-drug Interaction|Pharmacokinetics|Quizartinib Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. August 28 2020 Early Phase 1
NCT04209725 Terminated Drug: CPX-351|Drug: Quizartinib Leukemia Myeloid Acute SCRI Development Innovations LLC June 3 2020 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

技术支持

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操作手册

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常见问题及建议解决方法

问题 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.