Elimusertib (BAY-1895344)

Catalog No.S9864 Batch:S986401

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Technical Data

Formula

C20H21N7O
Molecular Weight 375.43 CAS No. 1876467-74-1
Solubility (25°C)* In vitro DMSO 17 mg/mL (45.28 mM)
Ethanol 3 mg/mL (7.99 mM)
Water Insoluble
* <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.)

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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

BAY-1895344 inhibits tumor cell growth and viability and exhibits potent antiproliferative activity in a broad spectrum of human tumor cell lines.[2]
In vivo

BAY 1895344 exhibits strong monotherapy efficacy in cancer xenograft models that carry DNA damage repair deficiencies.[2]

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 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.
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

Selleck's Elimusertib (BAY-1895344) has been cited by 6 publications

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
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
Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain [ J Med Chem, 2022, 65(5):4182-4200] PubMed: 35191694
Mismatch repair proteins play a role in ATR activation upon temozolomide treatment in MGMT-methylated glioblastoma [ Sci Rep, 2022, 12(1):5827] PubMed: 35388070
ATR inhibition enables complete tumour regression in ALK-driven NB mouse models [ Nat Commun, 2021, 12(1):6813] PubMed: 34819497

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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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