Berzosertib (VE-822)

For research use only. Not for use in humans.

目录号:S7102 别名: VX970,M6620

Berzosertib (VE-822) Chemical Structure

CAS No. 1232416-25-9

VE-822是一种ATR抑制剂,在HT29细胞中IC50 为 19 nM。

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客户使用Selleck生产的Berzosertib (VE-822)发表文献45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 VE-822是一种ATR抑制剂,在HT29细胞中IC50 为 19 nM。
特性 VE-822是在ATR抑制剂VE-821的高选择性和有效的衍生物。
靶点
ATR [1]
(HT29 cells)
19 nM
体外研究

作为对XRT和gemcitabine的响应,VE-822(80 nM)减弱ATR信号传导途径,并降低肿瘤细胞存活率。在正常细胞中,VE-822(80 nM)减弱ATR信号通路强度,但并没有增强辐射和gemcitabine杀伤正常细胞的能力。与XRT中的MiaPaCa-2和PSN-1细胞相比,VE-822(80 nM)增加XRT引起的残余γH2AX和53BP1灶。 在XRT中的MiaPaCa-2和PSN-1细胞,VE-822(80 nM)治疗前降低Rad51的焦点。VE-822(80 nM)单独增加MiaPaCa-2和PSN-1细胞停留在G1期的比率。VE-822(80 nM)降低MiaPaCa-2和PSN-1细胞中XRT丰富G2/M-phase-fraction。 VE-822单独作用不大,而VE-822(80 nM),XRT和/或gemcitabine和联用在PSN-1细胞中增强了早期和晚期的细胞凋亡。[1] VE-822增加了肿瘤对DNA损伤剂的反应,和pChk1 Ser345阻碍相关。

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCK1T-HPV16 NHGwcZNHfW6ldHnvckBCe3OjeR?= NVXodG9QOC53IH7N MWqyOEBpyqB? NYTCTJZJcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[gSVE> MWOyOVcyPzFyOB?=
HCK1T-HPV16 NH7XTINHfW6ldHnvckBCe3OjeR?= MoSzNE42KG6P NHHzfXczPCCqwrC= M4ezZ4VvcGGwY3XzJGUyNWSncHXu[IVvfCC{ZYDsbYNifGmxbjDv[kB1cGViSGDWNVYh\2Wwb33l NXy2Z5lQOjV5MUexNFg>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / AKT / p-AKT; 

PubMed: 29890208     


VE-822 treatment inhibited STAT3-AKT pathway activation in both KYSE70 and KYSE450.

p21 / caspase-3 / PARP / γ-H2AX; 

PubMed: 29890208     


Expression of several markers which reflects the cell proliferation or cell apoptosis or cell cycle progression or DNA damage was examined using western blotting. Caspase-3 and cleaved-PARP expression remarkably increased in cells exposure to combination of VE-822 and cisplatin. In the ATMdeficient cell, VE-822 combination with cisplatin more dramatic changes in the expression of p-AKT, p21, and γ-H2AX than control cells.

PARP / RPA32 / γH2AX / H4 / MEK; 

PubMed: 31014753     


(A and B) THP-1 (Panel A) and MOLM-13 (Panel B) cells were treated with VE-822 and AZD1775, alone or in combination for 24 h. Chromatin-bound RPA32 and γH2AX were analyzed by western blotting and probed with the indicated antibodies.

WEE1 / p-CDC25c / p-CDK1 / CDK1 / p-CDK2 / CDK2 / RRM1 / RRM2; 

PubMed: 31014753     


THP-1 and MOLM-13 cells were treated with VE-822, AZD1775, or VE + AZD for 24 h. Whole cell lysates were subjected to western blotting and probed with the indicated antibodies. The fold changes for the densitometry measurements, normalized to GAPDH and compared to the untreated control, are shown below the corresponding blot.

29890208 31014753
Growth inhibition assay
Cell viability; 

PubMed: 31014753     


AML cells were cultured in 96-well plates with 0, 0.125, 0.25, 0.5, 1, and 2 µM VE-822 for 72 h and cells were incubated with MTT.

31014753
Immunofluorescence
PD-L1 / Hsp90B1; 

PubMed: 30094103     


HeLa-GFP-PD-L1 cells were treated with cisplatin (10 μM) for 24 hours with or without VE-822 (0.1 μM) pretreatment, and PD-L1 localization was analyzed by immunofluorescence.

γH2AX / p53; 

PubMed: 29890208     


Combination treatment enhanced the DNA damage effect presented by examining fluorescence intensity of γ-H2A.X and p53 in ESCC cells. Cells treated with cisplatin, VE-822, or combination of two drugs for 24 h were fixed and co-labeled with anti -γH2AX and anti-p53 antibodies. The γ-H2A.X and p53 foci were analyzed by immunofluorescence microscopy. Combination treatment resulted in accumulation of DNA damage presented by stronger and more fluorescence staining of γ-H2AX and p53.

30094103 29890208
体内研究 VE-822(60毫克/千克)抑制在小鼠PSN-1肿瘤中丝氨酸345-Chk1的磷酸化。和XTR单独作用相比,VE-822(60毫克/千克)和XTR联用增加小鼠两PSN-1和的MiaPaCa-2肿瘤生长到XRT600 mm3的时间到2倍。和Gem+XRT1联用相比,VE-822(60毫克/千克)和gemcitabine,XRT联用大大延长了PSN-1肿瘤小鼠中肿瘤生长延迟。与XRT1相比VE-822(60毫克/千克)和XRT1联用增加摄取肿瘤44%,这表明添加VE-822增加了γH2AX的磷酸化和XRT所致的DNA损伤的持久性。[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)

动物实验:[1]
- 合并
  • Animal Models: 含PSN-1或MiaPaCa-2肿瘤的小鼠
  • Dosages: 60 毫克/千克
  • Administration: 口服灌胃
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 36 mg/mL (77.66 mM)
Water Insoluble
Ethanol Insoluble
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+45% PEG 300+H2O
11mg/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 463.55
化学式

C24H25N5O3S

CAS号 1232416-25-9
储存条件 粉状
溶于溶剂
别名 VX970,M6620

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
NCT02723864 Active not recruiting Drug: Veliparib + VX-970 + Cisplatin Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) August 9 2017 Phase 1
NCT02595931 Recruiting Drug: Berzosertib|Drug: Irinotecan Hydrochloride Metastatic Malignant Neoplasm|Refractory Malignant Neoplasm|Unresectable Malignant Neoplasm National Cancer Institute (NCI) June 8 2016 Phase 1
NCT02487095 Recruiting Drug: Topotecan|Drug: VX-970 (M6620) Carcinoma Non-Small -Cell Lung|Ovarian Neoplasms|Small Cell Lung Carcinoma|Uterine Cervical Neoplasms|Carcinoma Neuroendocrine|Extrapulmonary Small Cell Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 30 2015 Phase 1|Phase 2

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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:

    I want to have information to prepare VE-822 for mouse gavage. Thank you for your answer

  • 回答:

    VE-822 can be dissolved in 1% CMC Na at 30mg/ml as a suspension for oral gavage.

ATM/ATR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID