Elimusertib (BAY-1895344)

For research use only.

Catalog No.S9864

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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Biological Activity

Description 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.
Targets
ATR [1]
(Cell-free assay)
7 nM
In vitro

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

In vivo

BAY 1895344 exhibits strong monotherapy efficacy in cancer xenograft models that carry DNA damage repair deficiencies.[2]

Protocol

Cell Research:

[2]

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  • 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)
Animal Research:

[2]

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  • 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)

Solubility (25°C)

In vitro DMSO 17 mg/mL (45.28 mM)
Water Insoluble
Ethanol ''3 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 375.43
Formula

C20H21N7O

CAS No. 1876467-74-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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ATM/ATR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID