AZ20

For research use only. Not for use in humans.

目录号:S7050

AZ20 Chemical Structure

CAS No. 1233339-22-4

AZ20是一种新型有效的选择性ATR激酶抑制剂,无细胞试验中IC50为5 nM,比作用于mTOR的选择性高8倍。

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客户使用Selleck生产的AZ20发表文献32篇:

产品安全说明书

ATM/ATR抑制剂选择性比较

生物活性

产品描述 AZ20是一种新型有效的选择性ATR激酶抑制剂,无细胞试验中IC50为5 nM,比作用于mTOR的选择性高8倍。
特性 AZ20为首次报道的在体内显示出抑制肿瘤生长的ATR蛋白激酶抑制剂。
靶点
ATR [2]
(Cell-free assay)
mTOR [2]
(Cell-free assay)
5 nM 38 nM
体外研究

AZ20显示了对所有PI3K亚型与ATM和DNA-PK在一起的良好选择性。[2] 在体外,AZ20呈浓度依赖性降低pChk1 Ser345,pChk1 Ser317和pChk1 Ser296水平。延长AZ20的处理时间增加了γH2AX核染色,这是复制压力的表现。这和S期阻滞和增加的组蛋白H3的磷酸化相关。AZ20诱导体外的生长抑制和细胞死亡和它的的活性是和其它细胞毒性药物截然不同的。AZ2的细胞毒作用在和ATM 抑制剂KU-60019联用时提高。

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT29 M3rGUmZ2dmO2aX;uJIF{e2G7 M4G0flEhcHJ? M1zUSWlvcGmkaYTpc44hd2ZiQWTSMY1m\GmjdHXkJGNJUzFicHjvd5Bpd3K7bHH0bY9vKGG2IIPldolv\SB|NEWgbY4hcHWvYX6gTHQzQSClZXzsd{Bi\nSncjCxJIhzKGmwIIDy[ZNmdmOnIH;mJFQudmm2cn;xeYlvd2yrbnWgNU1wgGmmZTygTWM2OD1yLkC1{txO M2LCelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m0NlA2Lz5{M{O5OFIxPTxxYU6=
LoVo M1nYfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{LlNlczKGi{cx?= MnrrS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUI9XdyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUCuNu69VQ>? NGXFVW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5OFIxPSd-MkOzPVQzODV:L3G+
MDA-MB-468 M33Eb2Z2dmO2aX;uJIF{e2G7 NEL1PXNKdmirYnn0bY9vKG:oIH3UU3IudWWmaXH0[YQhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDDz[ZJqdmViNEezJIlvKGi3bXHuJG1FSS2PQj20Olgh[2WubIOsJGlEPTB;Mj60{txO NFrLV5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5OFIxPSd-MkOzPVQzODV:L3G+
LoVo M2jOeWFvfGm2dX3vdkBie3OjeR?= MVW1NEBu\y:tZx?= M3zsPFE{KGSjeYO= MnvQRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTH;Wc{Bk\WyuczD4[Y5w\3KjZoTl[EBqdiCVd3nzd{BvfS:wdTDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiCpcn;3eIghcW6qaXLpeIlwdiCjdDC1NEBu\y:tZzygdI8heWRiZn;yJFE{KGSjeYOgdoVt[XSrdnWgeI8h[2:wdILvcC=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7NEKwOUc,OjN|OUSyNFU9N2F-
LoVo M3O2PWFvfGm2dX3vdkBie3OjeR?= M3ixblI2KG2pL3vn NUTZRZpsOTNiZHH5dy=> NHnxemZCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMc3ZwKGOnbHzzJJhmdm:pcnHmeIVlKGmwIGP3bZN{KG63L371JI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IHfyc5d1cCCrbnjpZol1cW:wIHH0JFI2KG2pL3vnMEBxdyCkaXSg[o9zKDF|IHThfZMhemWuYYTpeoUhfG9iY3;ueJJwdA>? NInmOmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5OFIxPSd-MkOzPVQzODV:L3G+
HT29 MmPtSpVv[3Srb36gZZN{[Xl? M4q5VFYxKG2rboO= Mly3TY5pcWKrdHnvckBw\iCDVGKgbY4hcHWvYX6gTHQzQSClZXzsd{Bi\nSncjC2NEBucW6|IHL5JGhw\WOqc4SgN|MzPThic4ThbY5qdmdvYnHz[YQh[XO|YYmsJGlEPTB;MD6wOlHPxE1? MlzSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=
LoVo Mo[5R5l1d3SxeHnjbZR6KGG|c3H5 MX63NkBpenN? M{\VZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxwXm9iY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhT0l3ME2wMlLPxE1? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2Nke3Nkc,OzB|NE[3O|I9N2F-
MDA-MB-468 NWDBdo85TnWwY4Tpc44h[XO|YYm= NVOwNW5qUW6qaXLpeIlwdiCxZjDtWG9TKGmwIHj1cYFvKE2GQT3NRk01PjhiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gO|BUPktiU{KzOU8zOzZicHjvd5Bpd3K7bHH0bY9vNCCLQ{WwQVAvPzMQvF2= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2Nke3Nkc,OzB|NE[3O|I9N2F-
HT-29 MVrDfZRwfG:6aXPpeJkh[XO|YYm= NH7GepE4OiCqcoO= MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUCuPVfPxE1? NH\KeXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO0Olc4Oid-M{CzOFY4PzJ:L3G+
LoVo MlH6SpVv[3Srb36gZZN{[Xl? MYiyOUBu\y:tZx?= NV;tVlhoQCCqcoO= M1e0V3Bt[XOvYTDjc45k\W62cnH0bY9vKGmwIGP3bZN{KG63L371JI1wfXOnIIjlco9oemGodHXkJJdqfGhiaIXtZY4hVG:YbzDj[YxteyCjdDCyOUBu\y:tZzygdI8h[mmmIHHmeIVzKDhiaILzMEBEeD1zLklOwG0> M{LaclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{S2O|czLz5|MEO0Olc4OjxxYU6=
MDA-MB-468 NUe4[ZpDTnWwY4Tpc44h[XO|YYm= MYXJcohq[mm2aX;uJI9nKG2WT2KgbY4hcHWvYX6gUWRCNU2ELUS2PEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCDS2SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNicnXzbYR2\SxiSVO1NF0zNjUQvF2= MoK4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=
LoVo MVvGeY5kfGmxbjDhd5NigQ>? NGTnR5Y2OCCvZz;r[y=> MXG4JIhzew>? NIPXeYFRdGG|bXGgZ49v[2WwdILheIlwdiCrbjDTe4l{eyCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKEyxVn:gZ4VtdHNiYYSgOVAhdWdxa3esJJBwKHGmIHHmeIVzKDhiaILzMEBEeD1|LkZOwG0> MnXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
IC50; 

PubMed: 28176818     


(a and b) AML cell lines and primary patient samples were treated with variable concentrations of AZ20 in 96-well plates for 72 h and viable cells were determined using MTT reagent. IC50 values were calculated as drug concentration necessary to inhibit 50% OD590 compared to vehicle control treated cells. AML cell line data are graphed as mean values ± SEM from three independent experiments (panel a). For the patient samples, the IC50values are mean values of duplicates from one experiment due to limited sample. The horizontal lines indicate the median. (c) AML cell lines and primary patient sample AML#53 were treated with AZ20 for 24 h and then subjected to annexin V-FITC/PI staining and flow cytometry analyses. Mean percent annexin V + cells ± SEM from one representative experiment performed in triplicates are shown. For cell lines, experiments were repeated three times, while patient sample experiments were performed once due to limited available sample.

28176818
Western blot
p-CDK1 / CDK1 / p-CDK2 / CDK2 ; 

PubMed: 28176818     


OCI-AML3 and THP-1 cells were treated with 0–8 μM AZ20 for 24 h. Whole cell lysates were subjected to Western blotting and probed with the indicated antibodies. Densitometry measurements normalized to β-actin and then compared to vehicle control are presented. Western blots were repeated at least three times and one representative cropped blot is shown.

γH2AX / RRM1 / RRM2 ; 

PubMed: 28176818     


OCI-AML3 cells were treated with 8 μM AZ20 for 0, 2, 4, 8, 12 or 24 h. Whole cell lysates were subjecte d to Western blotting and probed with the indicated antibodies (panel c).

28176818
体内研究 LoVo肿瘤的雌性裸鼠口服AZ20,25毫克/公斤每天两次,或50毫克/公斤每天一次,服用13天显著抑制肿瘤生长。[2] 这是与异种移植组织中γH2AX的广泛的核染色持续升高有关,但在治疗剂量导致小鼠骨髓中瞬时升高,这表明AZ20的良好的治疗特性。sup>[1] AZ20是评估药物-药物潜在相互作用(DDI),特别是抑制细胞色素P450酶。 AZ20(10 μM)抑制细胞色素3A4介导的咪达唑仑的代谢,抑制率达50%。AZ20在大鼠PK研究中有良好的生物利用度。[2]

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)

动物实验:[2]
- 合并
  • Animal Models: LoVo大肠腺癌异种移植物
  • Dosages: 25 毫克/千克, 每天2次;50 毫克/千克, 每天1次
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 83 mg/mL (201.2 mM)
Ethanol 3 mg/mL (7.27 mM)
Water Insoluble

* 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 412.51
化学式

C21H24N4O3S

CAS号 1233339-22-4
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、SDS / 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、SDS / 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

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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:

    If I want to completely block the kinase activity from the in vitro cell lines, how much concentration I should use?

  • 回答:

    IC50 5nM was quoted from a previous publication in which the author tested IC50 of AZ20 in cell free assay. In cell culture, many factors, such as membrane permeability and target protein concentration, may affect the efficiency. Each cell line responses to the same compound differently and it is very difficult to predict the optimized concentration simply based on cell free data. In cell culture experiment, the required concentration is usually higher. We recommend that you perform a pilot experiment and test different concentrations (50nM to 500uM) to get the optimized condition.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID