Elimusertib (BAY-1895344)

For research use only. Not for use in humans.

目录号:S9864 中文名称:Elimusertib (BAY-1895344)

Elimusertib (BAY-1895344) Chemical Structure

CAS No. 1876467-74-1

Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM.

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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 Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM.
靶点
ATR [1]
(Cell-free assay)
7 nM
体外研究

BAY-1895344 inhibits tumor cell growth and viability and exhibits potent antiproliferative activity in a broad spectrum of human tumor cell lines.[2]

体内研究

BAY 1895344 exhibits strong monotherapy efficacy in cancer xenograft models that carry DNA damage repair deficiencies.[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)

细胞实验:

[2]

- 合并
  • Cell lines: HT-29 cells, M059J cells, 38 cancer cell lines
  • Concentrations: 3–300 nM
  • Incubation Time: 72 to 96 hours
  • Method:

    The antiproliferative activity of BAY 1895344 is evaluated against a panel of 38 cancer cell lines. Cell proliferation is measured after 72 to 96 hours of exposure to BAY1895344. Cell viability is determined using crystal violet staining or the CellTiter-Glo Cell Viability Assay.


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: female SCID beige mice, female C.B-17 SCID mice, male NMRI nude mice, female NMRI nude mice
  • Dosages: 50 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 17 mg/mL (45.28 mM)
Water Insoluble
Ethanol ''3 mg/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 375.43
化学式

C20H21N7O

CAS号 1876467-74-1
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

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04616534 Recruiting Procedure: Biopsy|Drug: Elimusertib|Drug: Gemcitabine Advanced Fallopian Tube Carcinoma|Advanced Malignant Solid Neoplasm|Advanced Ovarian Carcinoma|Advanced Pancreatic Adenocarcinoma|Advanced Primary Peritoneal Carcinoma|High Grade Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Metastatic Pancreatic Adenocarcinoma|Platinum-Resistant Fallopian Tube Carcinoma|Platinum-Resistant Ovarian Carcinoma|Platinum-Resistant Primary Peritoneal Carcinoma|Primary Peritoneal High Grade Serous Adenocarcinoma|Stage II Pancreatic Cancer AJCC v8|Stage IIA Pancreatic Cancer AJCC v8|Stage IIB Pancreatic Cancer AJCC v8|Stage III Fallopian Tube Cancer AJCC v8|Stage III Ovarian Cancer AJCC v8|Stage III Pancreatic Cancer AJCC v8|Stage III Primary Peritoneal Cancer AJCC v8|Stage IIIA Fallopian Tube Cancer AJCC v8|Stage IIIA Ovarian Cancer AJCC v8|Stage IIIA Primary Peritoneal Cancer AJCC v8|Stage IIIA1 Fallopian Tube Cancer AJCC v8|Stage IIIA1 Ovarian Cancer AJCC v8|Stage IIIA2 Fallopian Tube Cancer AJCC v8|Stage IIIA2 Ovarian Cancer AJCC v8|Stage IIIB Fallopian Tube Cancer AJCC v8|Stage IIIB Ovarian Cancer AJCC v8|Stage IIIB Primary Peritoneal Cancer AJCC v8|Stage IIIC Fallopian Tube Cancer AJCC v8|Stage IIIC Ovarian Cancer AJCC v8|Stage IIIC Primary Peritoneal Cancer AJCC v8|Stage IV Fallopian Tube Cancer AJCC v8|Stage IV Ovarian Cancer AJCC v8|Stage IV Pancreatic Cancer AJCC v8|Stage IV Primary Peritoneal Cancer AJCC v8|Stage IVA Fallopian Tube Cancer AJCC v8|Stage IVA Ovarian Cancer AJCC v8|Stage IVA Primary Peritoneal Cancer AJCC v8|Stage IVB Fallopian Tube Cancer AJCC v8|Stage IVB Ovarian Cancer AJCC v8|Stage IVB Primary Peritoneal Cancer AJCC v8|Unresectable Pancreatic Adenocarcinoma National Cancer Institute (NCI) February 12 2021 Phase 1
NCT04267939 Recruiting Drug: BAY1895344|Drug: Niraparib Advanced Solid Tumors (Excluding Prostate Cancer)|Ovarian Cancer Bayer February 26 2020 Phase 1
NCT04095273 Recruiting Drug: BAY1895344|Drug: Pembrolizumab Advanced Solid Tumors Bayer September 30 2019 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID