Home DNA Damage/DNA Repair ATM/ATR inhibitor Elimusertib (BAY-1895344) hydrochloride For research use only.

Elimusertib (BAY-1895344) hydrochloride

Synonyms: BAY-1895344 HCl

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

Elimusertib (BAY-1895344) hydrochloride Chemical Structure

CAS No.

Purity & Quality Control

Elimusertib (BAY-1895344) hydrochloride Related Products

Signaling Pathway

ATM/ATR Signaling Pathways

ATM/ATR Signaling Pathway

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

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 induced H2AX phosphorylation (IC50 = 36 nM)[1].
Cell Research Cell lines C4–2b and PC-3 cells
Concentrations 2 μM
Incubation Time 48 h
Method

Cells were treated with various concentrations of BAY1895344.
In Vivo
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].
Animal Research Animal Models C57BL/6N male mice
Dosages 40 mg/kg
Administration i.p.
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
NCT03188965 Completed
Advanced Solid Tumor|Non-Hodgkin''s Lymphoma|Mantle Cell Lymphoma
Bayer
 July 6 2017 Phase 1

Chemical Information & Solubility

Molecular Weight 411.89 Formula

C20H22ClN7O
CAS No. SDF Download Elimusertib (BAY-1895344) hydrochloride SDF
Smiles CC1COCCN1C2=NC3=C(C=CN=C3C4=CC=NN4)C(=C2)C5=CC=NN5C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 82 mg/mL ( (199.08 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 82 mg/mL

Ethanol : 82 mg/mL


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Elimusertib (BAY-1895344) hydrochloride | Elimusertib (BAY-1895344) hydrochloride supplier | purchase Elimusertib (BAY-1895344) hydrochloride | Elimusertib (BAY-1895344) hydrochloride cost | Elimusertib (BAY-1895344) hydrochloride manufacturer | order Elimusertib (BAY-1895344) hydrochloride | Elimusertib (BAY-1895344) hydrochloride distributor