Quizartinib (AC220)

For research use only. Not for use in humans.

目录号:S1526

Quizartinib (AC220) Chemical Structure

CAS No. 950769-58-1

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。

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 3026.14 现货
RMB 7933.51 现货
RMB 20229.3 现货
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客户使用Selleck生产的Quizartinib (AC220)发表文献67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 NHfaS|BHfW6ldHnvckBCe3OjeR?= MWKwMlEuOTBizszN NHn6dmE{OCCvaX6= NIXvNlFmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NVL0d|BIOjN7NkexO|c>
K562/ABCB1 M4D4VGZ2dmO2aX;uJGF{e2G7 MUGwMlEuOTBizszN NF;6b2E{OCCvaX6= MkPO[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M1nKV|I{QTZ5MUe3
8226/MR20  M{PNcWZ2dmO2aX;uJGF{e2G7 Mnu0NE4yNTFyIN88US=> NITIeWs{OCCvaX6= NFXPTXBmdmijbnPld{B2eHSja3Wgc4Yhe3Wkc4TyZZRmeyCxZjDBRmNIOiCjbnSgRWJESjFiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NV\GdmJKOjN7NkexO|c>
K562/ABCG2 NF;3[lFHfW6ldHnvckBCe3OjeR?= Mnz3NE4yNTFyIN88US=> MWKzNEBucW5? MnvE[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M1G4NVI{QTZ5MUe3
MCF-7 FLV1000 M3myN2tqdmG|ZTDBd5NigQ>? MYGw5qCUOzBiwsXN NIO0VZY2KG2rbh?= Mnjl[IVkemWjc3XzJHsyOjWLXT3JRWFRKHCqb4TvcIFj\Wyrbnegc4YhSUKFQkGgZZQhUUN3MDDv[kA{NjNizszN M{LnXlI{QTZ5MUe3
MCF-7 FLV1000 Moi4T4lv[XOnIFHzd4F6 NGCzeZcx6oDVM{CgxtVO M2nl[VUhdWmw M2m2d4Rm[3KnYYPld{BcOTJ3SW2tTWFCWCCyaH;0c4xi[mWuaX7nJI9nKEGEQ1KyJIF1KEmFNUCgc4YhOC5yNzFOwG0> M1jaXVI{QTZ5MUe3
K562/ABCG2 MmK3R4VtdCCYaXHibYxqfHliQYPzZZl{ NH64PFcxNjFxMD61M|EhyrWP NGTnNWY6PiCq Mnjid4Vve2m2aYrld{BMPTZ{L1HCR2czKGOnbHzzJJRwKG2rdH;4ZY51em:wZTD0c5BwfGWlYX9CpC=> NF;TfIUzOzl4N{G3Oy=>
8226/MR20 NHWz[GJE\WyuIG\pZYJqdGm2eTDBd5NigXN? NFjKOW4xNjFiwsXN M2C4W|k3KGh? NUXtTXNye2Wwc3n0bZpmeyCNNU[yM2FDS0d{IHPlcIx{KHSxIH3peI95[W62cn;u[UB1d3CxdHXjZY7DqA>? MXeyN|k3PzF5Nx?=
HMC1.1 M2fmV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrFTWM2OD1zNDDuUS=> NFPPfm0zOzR7N{OxOy=>
HMC1.2 M13lR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLtWnN[UUN3ME2xO|I4KG6P NXnWV4U4OjN2OUezNVc>
p815 NGL3WnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjMRVJKSzVyPUS0OUBvVQ>? MWmyN|Q6PzNzNx?=
Kasumi-1 NWXFS5F6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnCUI13UUN3ME2zOkBvVQ>? NUTLSW11OjN2OUezNVc>
M-07e + SCF NWrVVoN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;HTZpUUUN3ME23O{BvVQ>? MX[yN|Q6PzNzNx?=
EOL-1 M3P4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnrXINKSzVyPUGgcm0> NF7nOpczOzR7N{OxOy=>
MV4;11 Mnn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nJUmlEPTB:IEGgcm0> MXeyN|Q6PzNzNx?=
MOLM14 MlTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfWdY1kUUN3MEygNUBvVQ>? MojTNlM1QTd|MUe=
Pat.221 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorUTWM2OD14N{Wgcm0> M4PVUVI{PDl5M{G3
Pat.279 NEXrOXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXQe5k{UUN3ME2zOFM1KG6P MVmyN|Q6PzNzNx?=
Pat.299 NH\IWppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Ta[2lEPTB;N{K0PEBvVQ>? M2iwV|I{PDl5M{G3
Pat.305 NHzqV5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HZW2lEPTB;N{C3PUBvVQ>? M3q3R|I{PDl5M{G3
Pat.375 NWHlSHhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7JTlFKSzVyPUWwN{BvVQ>? NX;qPI5EOjN2OUezNVc>
Pat.379 M3rBTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPPOWlKSzVyPUiwOkBvVQ>? MljzNlM1QTd|MUe=
Pat.368 MmrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXHRolrUUN3ME2yO|AxKG6P NF7Ue5EzOzR7N{OxOy=>
Pat.601 NGHNUYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7CTWM2OD1zMUWzJI5O MoP4NlM1QTd|MUe=
HMC1.1 NWiybJA6SXCxcITvd4l{KEG|c3H5 NGDYPJVKSzVyPUOxJI5O NHX0O|MzOzR7N{OxOy=>
p815 NGPBRWZCeG:ydH;zbZMhSXO|YYm= NVTjVHdiUUN3ME2zOFEhdk1? NV7xT5JOOjN2OUezNVc>
Kasumi-1 NFPYcodCeG:ydH;zbZMhSXO|YYm= Mn\0TWM2OD14NzDuUS=> Mn\DNlM1QTd|MUe=
M-07e + SCF MnzORZBweHSxc3nzJGF{e2G7 M1\4[GlEPTB;N{igcm0> NXrkV2ZiOjN2OUezNVc>
EOL-1 NF7MO3JCeG:ydH;zbZMhSXO|YYm= M{LHdmlEPTB:IEGgcm0> Mn3zNlM1QTd|MUe=
MV4;11 M{\kZmFxd3C2b4Ppd{BCe3OjeR?= MlHpTWM2OD1{IH7N NGPlV2gzOzR7N{OxOy=>
MOLM14 MlrkRZBweHSxc3nzJGF{e2G7 M3vVUGlEPTB;MzDuUS=> MmHoNlM1QTd|MUe=
GIST822 NFjBUndCeG:ydH;zbZMhSXO|YYm= MorTTWM2OD1zMEmgcm0> MUKyN|Q6PzNzNx?=
Pat.368 M3jRTmFxd3C2b4Ppd{BCe3OjeR?= NF[wWJZKSzVyPUK5PVghdk1? NXHSdJlPOjN2OUezNVc>
Pat.601 MVXBdI9xfG:|aYOgRZN{[Xl? M3T4TWlEPTB;OEe2JI5O M2LCUVI{PDl5M{G3
MV4-11 NX;zXXlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLpO|IhcA>? NHjYRoFKSzVyPUCuN{BvVQ>? MV[yN|QyOjl|MR?=
MOLM-14 Ml2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nwSVczKGh? M3foTmlEPTB;MD6xJI5O M175b|I{PDF{OUOx
SEM-K2 NGXGSXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWi3NkBp NHzzR2dKSzVyPUCuOEBvVQ>? NX\uNFhpOjN2MUK5N|E>
RS4;11 M37jemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU[1fGl7PzJiaB?= NFnvWXJKSzVyPkGwMFAxOCCwTR?= M3zyNFI{PDF{OUOx
THP-1 NVL5TZJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[3NkBp NH;XO5JKSzVyPkGwMFAxOCCwTR?= NIr2VpozOzRzMkmzNS=>
MV4-11 NYC4RWZ6SXCxcITvd4l{KEG|c3H5 NULtfWlpQC9{NDDo MXfpcoR2[2W|IIPp[45q\mmlYX70JIFv\CCmb4PlMYRmeGWwZHXueEBRSVKSIHPs[YF3[WenIHHu[EBi[2O3bYXsZZRqd25ib3[gd5VjNTKQIFTORS=> MUSyN|QyOjl|MR?=
MOLM-14 MYDBdI9xfG:|aYOgRZN{[Xl? NGP3TZE5NzJ2IHi= M{HIS4lv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C MnXlNlM1OTJ7M{G=
SEM-K2 M3zGXGFxd3C2b4Ppd{BCe3OjeR?= MUi4M|I1KGh? NVTTSotKcW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? NV;0NZdFOjN2MUK5N|E>
MV4-11 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PKdVczKGh? NGj3WnVKSzVyPUCuOVYhyrFiMD6zJI5O MXGxPVY2PDRyOB?=
A375 NWi3NIw6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVO3NkBp Mke2TWM2OD5iMUCgNFAxKG6P MlfBNVk3PTR2MEi=

... Click to View More Cell Line Experimental Data

Assay
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]
- 合并

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]
- 合并
  • 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。
    (Only for Reference)
动物实验:[1]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 33 mg/mL (58.85 mM)
Water Insoluble
Ethanol Insoluble
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 粉状
溶于溶剂
别名 N/A

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04459585 Recruiting Drug: Dabigatran Etexilate Mesylate|Drug: Quizartinib Healthy Subjects|Drug-drug Interaction|Pharmacokinetics|Quizartinib Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. September 16 2020 Early Phase 1
NCT04459598 Recruiting Drug: Efavirenz|Drug: Quizartinib Healthy Subjects|Drug-drug Interaction|Pharmacokinetics|Quizartinib Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. September 9 2020 Early Phase 1
NCT04473664 Not yet recruiting Drug: Quizartinib Hepatic Impairment|Moderate Impaired Hepatic Function Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. September 23 2020 Phase 1
NCT04209725 Recruiting Drug: CPX-351|Drug: Quizartinib Leukemia Myeloid Acute SCRI Development Innovations LLC June 3 2020 Phase 2
NCT02984995 Completed Drug: Quizartinib Leukemia Myeloid Acute Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. December 8 2016 Phase 2

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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.

Target Protein Ligand Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID