受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C20H21N7O |
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分子量 | 375.43 | CAS No. | 1876467-74-1 | |
Solubility (25°C)* | 体外 | 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. |
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. |
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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] |
細胞アッセイ | 細胞株 | HT-29 cells, M059J cells, 38 cancer cell lines |
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濃度 | 3–300 nM | |
反応時間 | 72 to 96 hours | |
実験の流れ | 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. |
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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 |
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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 |
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。