Elimusertib (BAY-1895344) hydrochloride

Catalog No.S8666 Synonyms: BAY-1895344 HCl

For research use only.

Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.

Elimusertib (BAY-1895344) hydrochloride Chemical Structure

CAS No.

Selleck's Elimusertib (BAY-1895344) hydrochloride has been cited by 4 Publications

Purity & Quality Control

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Biological Activity

Description Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.
Targets
ATR [1]
(Cell-free assay)
7 nM
In vitro

In vitro, BAY 1895344 is shown to be a very potent and highly selective ATR inhibitor (IC50 = 7 nM), which potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC50 = 78 nM). In cellular mechanistic assays BAY 1895344 potently inhibits hydroxyurea-induced H2AX phosphorylation (IC50 = 36 nM)[1].

In vivo BAY 1895344 reveals significantly improved aqueous solubility, bioavailability across species and no activity in the hERG patch-clamp assay. It also demonstrates very promising efficacy in monotherapy in DNA damage deficient tumor models as well as combination treatment with DNA damage inducing therapies[1]. BAY 1895344 exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models of different indications that are characterized by DDR deficiencies, inducing stable disease in ovarian and colorectal cancer or even complete tumor remission in mantle cell lymphoma models[2].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 411.89
Formula

C20H22ClN7O

CAS No.
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1COCCN1C2=NC3=C(C=CN=C3C4=CC=NN4)C(=C2)C5=CC=NN5C

In vivo Formulation Calculator (Clear solution)

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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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05071209 Recruiting Drug: Elimusertib 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 3 2021 Phase 1|Phase 2
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|Fallopian Tube High Grade Serous Adenocarcinoma|Metastatic Pancreatic Adenocarcinoma|Ovarian High Grade Serous 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 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 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|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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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