Elimusertib (BAY-1895344) hydrochloride

Catalog No.S8666 Batch:S866602

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Technical Data

Formula

C20H22ClN7O
Molecular Weight 411.89 CAS No.
Solubility (25°C)* In vitro DMSO 82 mg/mL (199.08 mM)
Water 82 mg/mL (199.08 mM)
Ethanol 82 mg/mL (199.08 mM)
* <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) 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)

Cell Assay:

[3]
  • Cell lines

    C4–2b and PC-3 cells

  • Concentrations

    2 μM

  • Incubation Time

    48 h

  • Method

    Cells were treated with various concentrations of BAY1895344.
Animal Study:

[3]
  • Animal Models

    C57BL/6N male mice

  • Dosages

    40 mg/kg

  • Administration

    i.p.

Selleck's Elimusertib (BAY-1895344) hydrochloride has been cited by 8 publications

APOBEC3B coordinates R-loop to promote replication stress and sensitize cancer cells to ATR/Chk1 inhibitors [ Cell Death Dis, 2023, 14(6):348] PubMed: 37270643
Arginine shortage induces replication stress and confers genotoxic resistance by inhibiting histone H4 translation and promoting PCNA ubiquitination [ Cell Rep, 2023, 42(4):112296] PubMed: 36961817
The effect of inhibition of receptor tyrosine kinase AXL on DNA damage response in ovarian cancer [ Commun Biol, 2023, 6(1):660] PubMed: 37349576
Arginine shortage induces replication stress and confers genotoxic resistance by inhibiting histone H4 translation and promoting PCNA polyubiquitination [ bioRxiv, 2023, 2023.01.31.526362] PubMed: 36778247
Genetically Defined, Syngeneic Organoid Platform for Developing Combination Therapies for Ovarian Cancer [ Cancer Discov, 2021, 11(2):362-383] PubMed: 33158842
ATR inhibitor-induced CDK1-SPOP axis destabilizes PD-L1 and enhances cytotoxicity in prostate cancer [ Clin Cancer Res, 2021, clincanres.1010.2021] PubMed: 34168048
ATR/ATM-Mediated Phosphorylation of BRCA1 T1394 Promotes Homologous Recombinational Repair and G2-M Checkpoint Maintenance [ Cancer Res, 2021, 81(18):4676-4684] PubMed: 34301763
Double-strand breaks in ribosomal RNA genes activate a distinct signaling and chromatin response to facilitate nucleolar restructuring and repair [ Nucleic Acids Res, 2019, 10.1093/nar/gkz518] PubMed: 31184714

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.