Ceralasertib (AZD6738)

For research use only. Not for use in humans.

目录号:S7693

Ceralasertib (AZD6738) Chemical Structure

CAS No. 1352226-88-0

Ceralasertib (AZD6738) 是一种口服具有活性的,选择性 ATR 激酶抑制剂,IC50 为 1 nM。Phase 1/2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2432.43 现货
RMB 1615.57 现货
RMB 5700.55 现货
RMB 12039.3 现货
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客户使用Selleck生产的Ceralasertib (AZD6738)发表文献38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 Ceralasertib (AZD6738) 是一种口服具有活性的,选择性 ATR 激酶抑制剂,IC50 为 1 nM。Phase 1/2。
靶点
ATR [1]
(Cell-free assay)
1 nM
体外研究

在四个Kras突变细胞系:H23,H460,A549,和H358中,AZD6738抑制ATR激酶活性,并损害细胞活性。在ATM缺失的H23细胞中,AZD6738强烈增强顺铂诱导快速细胞死亡的作用。[1]在p53 或 ATM缺失的细胞中,AZD6738治疗引起复制叉停滞和未修复DNA损伤的积累,导致有丝分裂障碍,从而使细胞死亡。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LICR-LON-HN4 and LICR-LON-HN5 cells NXTpclg1TnWwY4Tpc44h[XO|YYm= Ml\CNE4xOyxiMD6xMEAxNjNuIEGsJFMtKDFyIN88US=> MmnTRXpFPjd|ODDpcohq[mm2aX;uJI9nKEGWUjD0bJJwfWeqIHzvd5Mhd2ZiZH;3cpN1emWjbTDwbI9{eGixconsZZRqd25ib3[gR2hMOSCxbjDT[ZI{PDVw MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3N{i5NEc,OzByNUe4PVA9N2F-
K8484 cells M3fHW2Z2dmO2aX;uJIF{e2G7 MlHJNkDPxE1? M3Gze|chcG:3coO= NVPRbXBuUW5iS{i0PFQh[2WubIOsJGFbTDZ5M{igZZQhOiEEtV2gZ49ueGyndHXsfUBxemW4ZX70[YQh\2WvY3n0ZYJqdmVvaX7keYNm\CCFaHuxJJBpd3OyaH;yfYxifGmxbjDvckBU\XKrbnWgN|Q2NCC2aHWg[I94dnO2cnXhcUBCXFJidHHy[4V1Ng>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh7MUS4PEc,Ojl6OUG0PFg9N2F-
SNU-601 cells NHjGZohE\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHzd4F6 Ml3NNE0yKM7:bX;sM2w> NWHYO4pEPSCmYYnz MWLUbIUhWyCjbnSgd5VjNUdzIIDvdJVt[XSrb37zJI9nKFOQVT22NFEh[2WubIOge4Vz\SCmcnHtZZRq[2GubImgZY5lKGSxc3Wt[IVx\W6mZX70cJkhcW6lcnXhd4VlKGK7IFHaSFY4Ozhw MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF|OECzOEc,OjhzM{iwN|Q9N2F-
breast cancer cell lines Mn74R4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjc4PhfS=> MWSwMlEzPSxiMD6yOUwhOC53IHHu[EAyNjBizszN NGDj[ZU2KGSjeYO= MYDJR|UxKH[jbIXld{Bz[W6pZXSg[pJwdSByLkOgeI8hRjFizsztc4wwVA>? Ml\NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MEGxNVMoRjJ5NUCxNVE{RC:jPh?=
LoVo cells M1njUGZ2dmO2aX;uJIF{e2G7 NGi3[4MzPCCq MV\S[YR2[3Srb36gbY4h[2WubDDjc5VvfDtiYTDwdo9xd3K2aX;uJI9nKHSqZTDj[YxtKHCxcIXsZZRqd25iYYLlJEhqdiCjZHTpeIlwdiC2bzDj[YxtKGO7Y3zlJIFzemW|dDmgeY5l\XKpb3nu[{BieG:ydH;zbZMhf2inbjDlfJBwe2WmIITvJIRzfWdiYYSgZ49v[2WwdILheIlwdnNiZ4LlZZRmeiC2aHHuJFPjiIoQvF2= M{nvUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{GwN|EzLz5{NkOxNFMyOjxxYU6=
HT29 cells NHHtPGJHfW6ldHnvckBie3OjeR?= M4nUb|YxKG2rboO= MX\JR|UxKD1iMD6wO|Qh|ryP NVvycYJmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOFY4PzJpPkOwN|Q3Pzd{PD;hQi=>
LoVo cells MUTDfZRwfG:6aXPpeJkh[XO|YYm= NY\POlhUPzJiaILz MXrHTVUxKD1iMD60OEDPxE1? M{DvVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{S2O|czLz5|MEO0Olc4OjxxYU6=
LoVo cells NIG4UFdHfW6ldHnvckBie3OjeR?= M3zY[VI2KG2pL3vn NVLsdpU4QCCqcoO= NXfvXYlHS3BiPTCwMlc1KM7:TR?= NVnuXWtORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOFY4PzJpPkOwN|Q3Pzd{PD;hQi=>
LoVo cells MmTUSpVv[3Srb36gZZN{[Xl? MVq1NEBu\y:tZx?= NEPucHA5KGi{cx?= MXLDdEA:KDJwMjFOwG0> NIPjO5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO0Olc4Oid-M{CzOFY4PzJ:L3G+
HT-29 cells M2DRbGN6fG:2b4jpZ4l1gSCjc4PhfS=> M2rmVVczKGi{cx?= M2\6VGdKPTBiPTCyMlYh|ryP M1TleVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{S2O|czLz5|MEO0Olc4OjxxYU6=
LoVo cells NYr5[oNETnWwY4Tpc44h[XO|YYm= Mo\NO|UhdWdxa3e= Mn3vPEBpenN? MWjDdEA:KDJwNjFOwG0> MlHPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=
MDA-MB-468 cells NYO5cmtUTnWwY4Tpc44h[XO|YYm= MWjJR|UxKD1iNT63JO69VQ>? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2Nke3Nkc,OzB|NE[3O|I9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pCHK1 / pCDC25c / pRPA32 / γH2AX / pHH3 / cleaved caspase-3 / RAD51; 

PubMed: 29605721     


MDA-231 or Hs578t cells were treated with 50 nM or 100 nM of AZD1775 with or without 500 nM of AZD6738 for 24 h. After treatment, western blot was performed using anti-γH2AX, anti-pCHK1 (S345), anti-CHK1, anti-pCDC25c (S216), anti-CDC25c, anti-pHH3, anti-RAD51 anti-pRPA32 (S4/S8), anti-cleaved-caspase 3, and anti-GAPDH antibodies. 

ATM pSer1981 / ATM / ATR / Chk1 pSer345 / Chk1 / Chk2 pThr68 / Chk2; 

PubMed: 26563132     


TP53/ATM wild-type (TP53/ATM-wt) primary CLL cells cocultured with and CLL cells, both CII-GFPsh and CII-ATMsh were treated with AZD6738 (1 μM) for 2 hours, or left untreated, prior to exposure to HU (1 mM) or IR (6 Gy) for a further 5 hours. AZD6738 treatment inhibited ATR signaling as indicated by a reduction in HU-induced Chk1 phosphorylation (lanes 3 vs 4 and 9 vs 10). In ATM-proficient CLL cells, this also led to ATM activation as evidenced by ATM phosphorylation and Chk2 phosphorylation (lane 3 vs 4). 

29605721 26563132
Immunofluorescence
γH2AX / RAD51; 

PubMed: 29605721     


MDA-231 cells were treated with 50 nM or 100 nM of AZD1775 with or without 500 nM of AZD6738 for 24 h. Cells were probed with anti-γH2AX and anti-RAD51 antibodies. Scale bar: 5 μm. 

53BP1; 

PubMed: 26563132     


Cells treated with AZD6738 (1 μM) for 48 hours were labeled with anti-53BP1 antibodies, and at least 200 cells were then analyzed in each sample using a ×60 lens. AZD6738 treatment led to an accumulation of 53BP1 foci in Mec1 and ATMi pretreated CII cells and an accumulation of 53BP1 bodies in CII cells without ATMi pretreatment.

29605721 26563132
Growth inhibition assay
Cell viability; 

PubMed: 26563132     


CII-GFPsh, CII-ATMsh (ATM-deficient), and Mec1 (p53-defective) cells were treated with AZD6738 for 4 days, and viability was measured using the CellTiter-Glo assay. Surviving fraction is expressed relative to untreated controls. AZD6738 induced significantly greater dose-dependent cytotoxicity with significantly lower AZD6738 EC50 in CII-ATMsh and Mec1 cells compared with CII-GFPsh cells.

IC50; 

PubMed: 28062704     


Cell line IC50 values assessed for growth inhibition in a 72-hour MTT assay

26563132 28062704
体内研究 在负荷H460和H23肿瘤的裸鼠中,AZD6738 (50 mg/kg, p.o.)导致肿瘤生长抑制(TGI),结合顺铂引起ATM缺失的H23肿瘤快速退化。[1]在负荷LoVo异种移植物的裸鼠中,AZD6738 (50 mg/kg) + IR (2 Gy)的组合避免了毒性,同时仍保持疗效。[3]

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)

细胞实验:[1]
- 合并
  • Cell lines: H23,H460,A549,和 H358 细胞
  • Concentrations: ~30 μM
  • Incubation Time: 48小时
  • Method: 细胞在白色壁,透明底的96孔板中与指示剂量的AZD6738,cisplatin,gemcitabine,或它们的组合处理48小时。ATP水平通过CellTiter-Glo发光细胞活性试验和Safire2酶标仪测量代替品活性评估。进一步分析之前,原始数据对本底发光进行校正。对于AZD6738治疗,在GraphPad Prism 6中将对数转化(x=log(x))的数据归一化为未处理对照组的平均值,通过非线性回归(log(抑制剂) vs. 对可变斜率的响应值) 生成对数剂量响应曲线。GI50值,定义为Y = 50%时,X的剂量,根据剂量反应曲线推导得出。
    (Only for Reference)
动物实验: [1]
- 合并
  • Animal Models: 负荷 H23 或 H460 异种移植物的雌性无胸腺裸鼠
  • Dosages: 25 或 50 mg/kg
  • Administration: p.o.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 82 mg/mL (198.78 mM)
Water Insoluble
Ethanol '41 mg/mL warmed
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):
5% DMSO+40% propylene glycol+ddH2O
10mg/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 412.51
化学式

C20H24N6O2S

CAS号 1352226-88-0
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
NCT04361825 Enrolling by invitation Drug: Durvalumab Small Cell Lung Cancer Samsung Medical Center|AstraZeneca June 17 2020 Phase 2
NCT04298008 Recruiting Drug: AZD6738|Drug: Durvalumab Bile Duct Cancer|Chemotherapy Effect Seoul National University Hospital June 25 2020 Phase 2
NCT04298021 Recruiting Drug: AZD6738|Drug: Durvalumab|Drug: Olaparib Bile Duct Cancer|Chemotherapy Effect Seoul National University Hospital June 25 2020 Phase 2
NCT03669601 Recruiting Drug: AZD6738|Drug: Gemcitabine Cancer CCTU- Cancer Theme|AstraZeneca|Cambridge University Hospitals NHS Foundation Trust October 15 2019 Phase 1
NCT03770429 Recruiting Drug: AZD6738 Leukemia|Myelodysplastic Syndrome Massachusetts General Hospital|AstraZeneca August 5 2019 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID