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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
10mM (1mL in DMSO)	RMB 2432.43	现货
5mg	RMB 1615.57	现货
25mg	RMB 5700.55	现货
100mg	RMB 12039.3	现货
大包装	有超大折扣

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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

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=

Click to View More Cell Line Experimental Data

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]

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.

参考文献	[1] Vendetti FP, et al. Oncotarget. 2015. doi: 10.18632/oncotarget.6247. [2] Kwok M, et al. Lancet. 2015. doi: 10.1016/S0140-6736(15)60373-7. [3] Checkley S, et al. Sci Rep. 2015. doi: 10.1038/srep13545.

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
储存条件	2年	-80°C	溶于溶剂

Download Ceralasertib (AZD6738) SDF

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 μL 动物数量只

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，注：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：取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：取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
=	×	×

稀释计算器分子量计算器

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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