Elimusertib (BAY-1895344)

製品コードS9864 バッチS986402

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₀H₂₁N₇O

分子量

375.43

CAS No.

1876467-74-1

Solubility (25°C)*

体外

DMSO

25 mg/mL (66.59 mM)

Ethanol

4 mg/mL (10.65 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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.^[2]
in vivo	Elimusertib (BAY-1895344) exhibits strong monotherapy efficacy in cancer xenograft models that carry DNA damage repair deficiencies.^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HT-29 cells, M059J cells, 38 cancer cell lines
	濃度	3–300 nM
	反応時間	72 to 96 hours
	実験の流れ	Elimusertib (BAY-1895344) is evaluated for its antiproliferative activity against a panel of 38 cancer cell lines. Cell proliferation is measured after 72 to 96 hours of exposure to this compound, and viability is determined using crystal violet staining or the CellTiter-Glo Cell Viability Assay.
動物実験	動物モデル	female SCID beige mice, female C.B-17 SCID mice, male NMRI nude mice, female NMRI nude mice
	投薬量	50 mg/kg
	投与方法	Oral gavage

参考

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
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
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
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
Protection of nascent DNA at stalled replication forks is mediated by phosphorylation of RIF1 intrinsically disordered region [ Elife, 2022, 11e75047]	PubMed: 35416772

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。