Elimusertib (BAY 1895344)

Catalog No.S9864 Batch:S986402

Technical Data

Formula

C₂₀H₂₁N₇O

Molecular Weight

375.43

CAS No.

1876467-74-1

Solubility (25°C)*

In vitro

DMSO

25 mg/mL (66.59 mM)

Ethanol

4 mg/mL (10.65 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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.

Protocol (from reference)

Cell Assay:^{^[2]}	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 Elimusertib (BAY-1895344) is evaluated against a panel of 38 cancer cell lines. After 72 to 96 hours of exposure to this compound, cell proliferation is measured. Cell viability is determined using crystal violet staining or the CellTiter-Glo Cell Viability Assay.
Animal Study:^{^[2]}	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

Cell Assay:^{^[2]}

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 Elimusertib (BAY-1895344) is evaluated against a panel of 38 cancer cell lines. After 72 to 96 hours of exposure to this compound, cell proliferation is measured. Cell viability is determined using crystal violet staining or the CellTiter-Glo Cell Viability Assay.

Animal Study:^{^[2]}

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

References

https://cancerres.aacrjournals.org/content/77/13_Supplement/983
https://pubmed.ncbi.nlm.nih.gov/31582533/

Selleck's Elimusertib (BAY 1895344) Has Been Cited by 14 Publications

REV7 functions with REV3 as a checkpoint protein delaying mitotic entry until DNA replication is completed [ Cell Rep, 2025, 44(4):115431]	PubMed: 40106439
Enhancing PDAC therapy: Decitabine-olaparib synergy targets KRAS-dependent tumors [ iScience, 2025, 28(2):111842]	PubMed: 40008360
ATR Inhibition Synergizes With Alkylating PI Polyamide Targeting MYCN by Suppressing DNA Repair in MYCN-Amplified Neuroblastoma [ Cancer Sci, 2025, 10.1111/cas.70043]	PubMed: 40052411
MGMT function determines the differential response of ATR inhibitors with DNA-damaging agents in glioma stem cells for GBM therapy [ Neuro-Oncology Advances, 2024, vdad165]	PubMed: 38213834.0
Epigenetic targeting of PGBD5-dependent DNA damage in SMARCB1-deficient sarcomas [ bioRxiv, 2024, 2024.05.03.592420]	PubMed: 38766189
MGMT function determines the differential response of ATR inhibitors with DNA-damaging agents in glioma stem cells for GBM therapy [ Neurooncol Adv, 2024, 6(1):vdad165]	PubMed: 38213834
The suppression of ATR/Chk1 pathway by Elimusertib ATR inhibitor in triple negative breast cancer cells [ American Journal of Translational Research, 2023, 4902-4911]	PubMed: 37560219.0
A biscarbene gold(I)-NHC-complex overcomes cisplatin-resistance in A2780 and W1 ovarian cancer cells highlighting pERK as regulator of apoptosis [ Cancer Chemother Pharmacol, 2023, 92(1):57-69]	PubMed: 37272932
The suppression of ATR/Chk1 pathway by Elimusertib ATR inhibitor in triple negative breast cancer cells [ Am J Transl Res, 2023, 15(7):4902-4911]	PubMed: 37560219
RUVBL1 and RUVBL2 as Novel Druggable DNA Damage Response Regulators in the N-Myc Regulatory Network in Neuroblastoma [ Research Square, 2023, Version 1]	PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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