Ceralasertib (AZD6738)

目录号:S7693

仅限科研使用

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。

Ceralasertib (AZD6738) Chemical Structure

CAS: 1352226-88-0

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69篇:

产品安全说明书

ATM/ATR抑制剂选择性比较

相关ATM/ATR产品

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 NWHIUlViTnWwY4Tpc44h[XO|YYm= MkfTNE4xOyxiMD6xMEAxNjNuIEGsJFMtKDFyIN88US=> NX;rT3hSSVqGNkezPEBqdmirYnn0bY9vKG:oIFHUVkB1cHKxdXfoJIxwe3Nib3[g[I94dnO2cnXhcUBxcG:|cHjvdplt[XSrb36gc4YhS0iNMTDvckBU\XJ|NEWu MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3N{i5NEc,OzByNUe4PVA9N2F-
K8484 cells M4HjdWZ2dmO2aX;uJIF{e2G7 M1OzOFIh|ryP NVvyfZhbPyCqb4Xydy=> NF3LS3VKdiCNOES4OEBk\WyuczygRXpFPjd|ODDheEAzKML3TTDjc41xdGW2ZXz5JJBz\X[nboTl[EBo\W2laYThZolv\S2rbnT1Z4VlKEOqa{GgdIhwe3Cqb4L5cIF1cW:wIH;uJHNmemmwZTCzOFUtKHSqZTDkc5dve3S{ZXHtJGFVWiC2YYLn[ZQv Mk\HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6OUG0PFgoRjJ7OEmxOFg5RC:jPh?=
SNU-601 cells NYDKUYlyS2WubDDndo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGjwVZQxNTFizsztc4wwVA>? NX;WeWh7PSCmYYnz NYjMXlRUXGinIGOgZY5lKHO3Yj3HNUBxd3C3bHH0bY9veyCxZjDTUnUuPjBzIHPlcIx{KHencnWg[JJidWG2aXPhcIx6KGGwZDDkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnZDDifUBCYkR4N{O4Mi=> NX3IcmlIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixN|gxOzRpPkK4NVM5ODN2PD;hQi=>
breast cancer cell lines MUDD[YxtKGe{b4f0bEBqdmirYnn0bY9vKGG|c3H5 NVrFTFA3OC5zMkWsJFAvOjVuIECuOUBidmRiMT6wJO69VQ>? NHr6fnc2KGSjeYO= NE\OXVlKSzVyII\hcJVmeyC{YX7n[YQh\nKxbTCwMlMhfG9iPkGg{txud2xxTB?= Moq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MEGxNVMoRjJ5NUCxNVE{RC:jPh?=
LoVo cells M2fJR2Z2dmO2aX;uJIF{e2G7 M3XzNFI1KGh? M4DYTHJm\HWldHnvckBqdiClZXzsJINwfW62OzDhJJBzd3CxcoTpc44hd2ZidHjlJINmdGxicH;weYxifGmxbjDhdoUhMGmwIHHk[Il1cW:wIITvJINmdGxiY4njcIUh[XK{ZYP0LUB2dmSncnfvbY5oKGGyb4D0c5NqeyC5aHXuJIV5eG:|ZXSgeI8h\HK3ZzDheEBkd26lZX70doF1cW:wczDndoVifGW{IIToZY4hO+LCid88US=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjNzMEOxNkc,OjZ|MUCzNVI9N2F-
HT29 cells MVvGeY5kfGmxbjDhd5NigQ>? MkjkOlAhdWmwcx?= MliyTWM2OCB;IECuNFc1KM7:TR?= MlTiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=
LoVo cells M{fpSGN6fG:2b4jpZ4l1gSCjc4PhfS=> M1qwe|czKGi{cx?= MkmwS2k2OCB;IECuOFQh|ryP M2HlclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{S2O|czLz5|MEO0Olc4OjxxYU6=
LoVo cells Mnm2SpVv[3Srb36gZZN{[Xl? M2LVdFI2KG2pL3vn MkTGPEBpenN? NEP1XnREeCB;IECuO|Qh|ryP NG\oeW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO0Olc4Oid-M{CzOFY4PzJ:L3G+
LoVo cells M1uwXmZ2dmO2aX;uJIF{e2G7 M1zMSFUxKG2pL3vn NWXSeFl6QCCqcoO= NWnKTmVJS3BiPTCyMlIh|ryP NG[0So09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO0Olc4Oid-M{CzOFY4PzJ:L3G+
HT-29 cells M3i5NWN6fG:2b4jpZ4l1gSCjc4PhfS=> NUfTb4ZuPzJiaILz M1jZPWdKPTBiPTCyMlYh|ryP MoTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=
LoVo cells NXXLRm9ETnWwY4Tpc44h[XO|YYm= M{\hTFc2KG2pL3vn MXG4JIhzew>? MXHDdEA:KDJwNjFOwG0> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2Nke3Nkc,OzB|NE[3O|I9N2F-
MDA-MB-468 cells NWDNT|FxTnWwY4Tpc44h[XO|YYm= MoGzTWM2OCB;IEWuO{DPxE1? M1PFXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{S2O|czLz5|MEO0Olc4OjxxYU6=
Assay
Methods Test Index PMID
Western blot ATM pSer1981 / ATM / ATR / Chk1 pSer345 / Chk1 / Chk2 pThr68 / Chk2 pCHK1 / pCDC25c / pRPA32 / γH2AX / pHH3 / cleaved caspase-3 / RAD51 26563132 29605721
Immunofluorescence 53BP1 γH2AX / RAD51 26563132 29605721
Growth inhibition assay IC50 Cell viability 28062704 26563132
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]
  • 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。
动物实验: [1]
  • 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.

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):
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 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
NCT05450692 Not yet recruiting Drug: Ceralasertib|Drug: Durvalumab|Drug: Docetaxel Advanced or Metastatic Non-Small Cell Lung Cancer AstraZeneca|Parexel September 15 2022 Phase 3
NCT05061134 Not yet recruiting Drug: Ceralasertib|Biological: Durvalumab Melanoma AstraZeneca July 11 2022 Phase 2
NCT05469919 Recruiting Drug: Ceralasertib Advanced Solid Malignancies AstraZeneca June 9 2022 Phase 1
NCT04704661 Recruiting Drug: Ceralasertib|Biological: Trastuzumab Deruxtecan Advanced Breast Carcinoma|Advanced Colon Carcinoma|Advanced Colorectal Carcinoma|Advanced Endometrial Carcinoma|Advanced Gastric Carcinoma|Advanced Gastroesophageal Junction Adenocarcinoma|Advanced Malignant Solid Neoplasm|Advanced Salivary Gland Carcinoma|Anatomic Stage III Breast Cancer AJCC v8|Anatomic Stage IIIA Breast Cancer AJCC v8|Anatomic Stage IIIB Breast Cancer AJCC v8|Anatomic Stage IIIC Breast Cancer AJCC v8|Anatomic Stage IV Breast Cancer AJCC v8|Clinical Stage III Gastric Cancer AJCC v8|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IV Gastric Cancer AJCC v8|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IVA Gastric Cancer AJCC v8|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IVB Gastric Cancer AJCC v8|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8|HER2-Positive Breast Carcinoma|Malignant Hepatobiliary Neoplasm|Metastatic Breast Carcinoma|Metastatic Gastroesophageal Junction Adenocarcinoma|Metastatic Malignant Solid Neoplasm|Pathologic Stage III Gastric Cancer AJCC v8|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIA Gastric Cancer AJCC v8|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIB Gastric Cancer AJCC v8|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIC Gastric Cancer AJCC v8|Pathologic Stage IV Gastric Cancer AJCC v8|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8|Prognostic Stage III Breast Cancer AJCC v8|Prognostic Stage IIIA Breast Cancer AJCC v8|Prognostic Stage IIIB Breast Cancer AJCC v8|Prognostic Stage IIIC Breast Cancer AJCC v8|Prognostic Stage IV Breast Cancer AJCC v8|Stage III Colon Cancer AJCC v8|Stage III Colorectal Cancer AJCC v8|Stage III Major Salivary Gland Cancer AJCC v8|Stage III Uterine Corpus Cancer AJCC v8|Stage IIIA Colon Cancer AJCC v8|Stage IIIA Colorectal Cancer AJCC v8|Stage IIIA Uterine Corpus Cancer AJCC v8|Stage IIIB Colon Cancer AJCC v8|Stage IIIB Colorectal Cancer AJCC v8|Stage IIIB Uterine Corpus Cancer AJCC v8|Stage IIIC Colon Cancer AJCC v8|Stage IIIC Colorectal Cancer AJCC v8|Stage IIIC Uterine Corpus Cancer AJCC v8|Stage IIIC1 Uterine Corpus Cancer AJCC v8|Stage IIIC2 Uterine Corpus Cancer AJCC v8|Stage IV Colon Cancer AJCC v8|Stage IV Colorectal Cancer AJCC v8|Stage IV Major Salivary Gland Cancer AJCC v8|Stage IV Uterine Corpus Cancer AJCC v8|Stage IVA Colon Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVA Major Salivary Gland Cancer AJCC v8|Stage IVA Uterine Corpus Cancer AJCC v8|Stage IVB Colon Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVB Major Salivary Gland Cancer AJCC v8|Stage IVB Uterine Corpus Cancer AJCC v8|Stage IVC Colon Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8|Stage IVC Major Salivary Gland Cancer AJCC v8|Unresectable Colorectal Carcinoma|Unresectable Gastroesophageal Junction Adenocarcinoma|Unresectable Malignant Solid Neoplasm National Cancer Institute (NCI) March 5 2021 Phase 1
NCT04361825 Enrolling by invitation Drug: Durvalumab Small Cell Lung Cancer Samsung Medical Center|AstraZeneca June 17 2020 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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