Home PI3K/Akt/mTOR ATM/ATR inhibitor Elimusertib (BAY-1895344)

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Elimusertib (BAY-1895344) ATM/ATR inhibitor

Cat.No.S9864

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

Chemical Structure

Molecular Weight: 375.43

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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 17 mg/mL (45.28 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

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In vivo
Batch:

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 375.43 Formula

C20H21N7O

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1876467-74-1 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1COCCN1C2=CC(=C3C=CN=C(C4=CC=N[NH]4)C3=N2)C5=CC=N[N]5C

Mechanism of Action

Targets/IC50/Ki
ATR
(Cell-free assay)
7 nM
In vitro

Elimusertib (BAY-1895344) inhibits tumor cell growth and viability and exhibits potent antiproliferative activity in a broad spectrum of human tumor cell lines.
In vivo

In cancer xenograft models with DNA damage repair deficiencies, Elimusertib (BAY-1895344) exhibits strong monotherapy efficacy.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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