Home PI3K/Akt/mTOR ATM/ATR inhibitor Elimusertib (BAY-1895344) For research use only.

Elimusertib (BAY-1895344)

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.

Elimusertib (BAY-1895344) Chemical Structure

Elimusertib (BAY-1895344) Chemical Structure

CAS No. 1876467-74-1

Purity & Quality Control

Elimusertib (BAY-1895344) Related Products

Signaling Pathway

ATM/ATR Signaling Pathways

ATM/ATR Signaling Pathway

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
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]
Cell Research 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.
In Vivo
In vivo

BAY 1895344 exhibits strong monotherapy efficacy in cancer xenograft models that carry DNA damage repair deficiencies.[2]
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05071209 Active not recruiting
Recurrent Alveolar Rhabdomyosarcoma|Recurrent Ewing Sarcoma|Recurrent Lymphoma|Recurrent Malignant Solid Neoplasm|Refractory Alveolar Rhabdomyosarcoma|Refractory Ewing Sarcoma|Refractory Lymphoma|Refractory Malignant Solid Neoplasm
National Cancer Institute (NCI)
 December 22 2021 Phase 1|Phase 2
NCT04267939 Terminated
Advanced Solid Tumors (Excluding Prostate Cancer)|Ovarian Cancer
Bayer|GlaxoSmithKline
 February 26 2020 Phase 1

Chemical Information & Solubility

Molecular Weight 375.43 Formula

C20H21N7O
CAS No. 1876467-74-1 SDF --
Smiles CC1COCCN1C2=CC(=C3C=CN=C(C4=CC=N[NH]4)C3=N2)C5=CC=N[N]5C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 17 mg/mL ( (45.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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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.

Handling Instructions

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