Quizartinib (AC220)

目录号:S1526

Quizartinib (AC220) Chemical Structure

Molecular Weight(MW): 560.67

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。Phase 3。

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RMB 2891.02 现货
RMB 1729.76 现货
RMB 3026.14 现货
RMB 7933.51 现货
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客户使用该产品的4个实验数据:

  • 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.

产品安全说明书

FLT3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。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 MonHSpVv[3Srb36gRZN{[Xl? NVHKeodNOC5zLUGwJO69VQ>? MmLLN|AhdWmw MYjlcohidmOnczD1dJRic2Vib3[gd5Vje3S{YYTld{Bw\iCDQlPHNkBidmRiQVLDRlEhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MXWyN|k3PzF5Nx?=
K562/ABCB1 NEHw[IpHfW6ldHnvckBCe3OjeR?= NWLRV21LOC5zLUGwJO69VQ>? NUS4eGgzOzBibXnu MknN[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MnOzNlM6PjdzN{e=
8226/MR20  NGf6[4dHfW6ldHnvckBCe3OjeR?= NWrtcZFUOC5zLUGwJO69VQ>? MlnEN|AhdWmw M2e5[IVvcGGwY3XzJJVxfGGtZTDv[kB{fWK|dILheIV{KG:oIFHCR2czKGGwZDDBRmNDOSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NIPoXXczOzl4N{G3Oy=>
K562/ABCG2 NIfoS3RHfW6ldHnvckBCe3OjeR?= MYKwMlEuOTBizszN NFPxV3c{OCCvaX6= MmHM[Y5p[W6lZYOgeZB1[WunIH;mJJN2[nO2cnH0[ZMhd2ZiQVLDS|Ih[W6mIFHCR2IyKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M2PyVVI{QTZ5MUe3
MCF-7 FLV1000 MmnUT4lv[XOnIFHzd4F6 NE\4W5gx6oDVM{CgxtVO M{XUSFUhdWmw NWDPNGV{\GWlcnXhd4V{KFtzMkXJYU1KSUGSIIDoc5RwdGGkZXzpcochd2ZiQVLDRlEh[XRiSVO1NEBw\iB|LkOg{txO NILhfI8zOzl4N{G3Oy=>
MCF-7 FLV1000 MYTLbY5ie2ViQYPzZZk> NEXKSFgx6oDVM{CgxtVO M1q3VlUhdWmw MmD4[IVkemWjc3XzJHsyOjWLXT3JRWFRKHCqb4TvcIFj\Wyrbnegc4YhSUKFQkKgZZQhUUN3MDDv[kAxNjB5IN88US=> MlXFNlM6PjdzN{e=
K562/ABCG2 MmrlR4VtdCCYaXHibYxqfHliQYPzZZl{ MlvRNE4yNzBwNT:xJOK2VQ>? Ml6xPVYhcA>? MnXCd4Vve2m2aYrld{BMPTZ{L1HCR2czKGOnbHzzJJRwKG2rdH;4ZY51em:wZTD0c5BwfGWlYX9CpC=> NW\lVGE2OjN7NkexO|c>
8226/MR20 M1LGTmNmdGxiVnnhZoltcXS7IFHzd4F6ew>? NG[1UGMxNjFiwsXN NHvkTI06PiCq M3;5RpNmdnOrdHn6[ZMhUzV4Mj;BRmNIOiClZXzsd{B1dyCvaYTvfIFvfHKxbnWgeI9xd3SnY3HuxsA> MkK5NlM6PjdzN{e=
HMC1.1 NXfzdnIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTF2IH7N NGD6SmIzOzR7N{OxOy=>
HMC1.2 M2rZfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmKxTWM2OD1zN{K3JI5O NVXNZ3I5OjN2OUezNVc>
p815 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[3TWM2OD12NEWgcm0> NYnSbmY5OjN2OUezNVc>
Kasumi-1 NESzWnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTN4IH7N M162Z|I{PDl5M{G3
M-07e + SCF M{TNS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3X1XWlEPTB;N{egcm0> NVvFZ4lVOjN2OUezNVc>
EOL-1 M4D6[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLMTnZKSzVyPUGgcm0> M1ruNFI{PDl5M{G3
MV4;11 NUG3SGZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPzXZN{UUN3MEygNUBvVQ>? MYCyN|Q6PzNzNx?=
MOLM14 MoLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRCBzIH7N NYnpfoU5OjN2OUezNVc>
Pat.221 M1TIXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTZ5NTDuUS=> MUCyN|Q6PzNzNx?=
Pat.279 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTN2M{Sgcm0> NYXOfXU2OjN2OUezNVc>
Pat.299 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTd{NEigcm0> MoPLNlM1QTd|MUe=
Pat.305 MoPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTdyN{mgcm0> MVKyN|Q6PzNzNx?=
Pat.375 NHrHNHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrnWHp7UUN3ME21NFMhdk1? M2G4dlI{PDl5M{G3
Pat.379 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nkSGlEPTB;OEC2JI5O MnqwNlM1QTd|MUe=
Pat.368 NVS5NGd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTJ5MECgcm0> MWqyN|Q6PzNzNx?=
Pat.601 MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;zTWM2OD1zMUWzJI5O MVKyN|Q6PzNzNx?=
HMC1.1 NX:4eVFkSXCxcITvd4l{KEG|c3H5 M3TUUWlEPTB;M{Ggcm0> NF60d44zOzR7N{OxOy=>
p815 M3nzNGFxd3C2b4Ppd{BCe3OjeR?= M3LRNWlEPTB;M{SxJI5O NIH2S4EzOzR7N{OxOy=>
Kasumi-1 NXHQRW5ZSXCxcITvd4l{KEG|c3H5 NV\RRWhQUUN3ME22O{BvVQ>? MVeyN|Q6PzNzNx?=
M-07e + SCF MlnuRZBweHSxc3nzJGF{e2G7 NVzCdYw{UUN3ME23PEBvVQ>? NWfVU5Z5OjN2OUezNVc>
EOL-1 NFvSUXFCeG:ydH;zbZMhSXO|YYm= Mmi2TWM2ODxiMTDuUS=> M{\yOlI{PDl5M{G3
MV4;11 MYrBdI9xfG:|aYOgRZN{[Xl? NYjQOWV5UUN3ME2yJI5O MkniNlM1QTd|MUe=
MOLM14 NYTBVGRMSXCxcITvd4l{KEG|c3H5 NFficINKSzVyPUOgcm0> MVqyN|Q6PzNzNx?=
GIST822 MVHBdI9xfG:|aYOgRZN{[Xl? M4npfmlEPTB;MUC5JI5O NEi1b48zOzR7N{OxOy=>
Pat.368 NYnpe21bSXCxcITvd4l{KEG|c3H5 M1HzN2lEPTB;Mkm5PEBvVQ>? M{j3NlI{PDl5M{G3
Pat.601 MnjGRZBweHSxc3nzJGF{e2G7 NWTmSYhJUUN3ME24O|Yhdk1? M3u1UVI{PDl5M{G3
MV4-11 NH7Hc|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPDOFNYPzJiaB?= NWDJcI1NUUN3ME2wMlMhdk1? NX\sbo81OjN2MUK5N|E>
MOLM-14 MmTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{j2[lczKGh? NUPUVoJbUUN3ME2wMlEhdk1? MYSyN|QyOjl|MR?=
SEM-K2 NXHBV4g5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PFOVczKGh? M33wdGlEPTB;MD60JI5O NHLyWogzOzRzMkmzNS=>
RS4;11 NWH2OXRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{ntbVczKGh? MlrwTWM2OD5zMDywNFAhdk1? MVSyN|QyOjl|MR?=
THP-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzyXXJrPzJiaB?= NYjpW4o{UUN3ME6xNEwxODBibl2= MlHGNlM1OTJ7M{G=
MV4-11 MVnBdI9xfG:|aYOgRZN{[Xl? NFSwNlI5NzJ2IHi= NVHVVVFbcW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? MoCyNlM1OTJ7M{G=
MOLM-14 NGjTZ4xCeG:ydH;zbZMhSXO|YYm= MVO4M|I1KGh? NUT5OZQ6cW6mdXPld{B{cWewaX\pZ4FvfCCjbnSg[I9{\S2mZYDlcoRmdnRiUFHSVEBkdGWjdnHn[UBidmRiYXPjeY12dGG2aX;uJI9nKHO3Yj2yUkBFVkF? MXSyN|QyOjl|MR?=
SEM-K2 M4\KSWFxd3C2b4Ppd{BCe3OjeR?= MnrlPE8zPCCq M3zITIlv\HWlZYOgd4lodmmoaXPhcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KFCDUmCgZ4xm[X[jZ3WgZY5lKGGlY4XteYxifGmxbjDv[kB{fWJvMl6gSG5C NF[wfm4zOzRzMkmzNS=>
MV4-11 Mk[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[3NkBp M{T4NWlEPTB;MD61OkDDuSByLkOgcm0> NHjOOHYyQTZ3NESwPC=>
A375 NGnXeVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVK3NkBp NITtdIlKSzVyPjCxNEAxODBibl2= M{PaUFE6PjV2NEC4

... Click to View More Cell Line Experimental Data

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]
+ 展开

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]
+ 展开
  • 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]
+ 展开
  • Animal Models: 雌性裸鼠或严重联合免疫缺陷鼠
  • Formulation: 22%羟丙基-β-环糊精
  • 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 从左到右依次加入纯溶剂:
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
稳定性 powder
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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 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

技术支持

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID