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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | ||||
化学式 | C46H47ClN8O9S |
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分子量 | 923.43 | CAS No. | 1818885-28-7 | ||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (108.29 mM) | ||||
Ethanol | 6 mg/mL (6.49 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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 | ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC. |
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in vitro | Compared with the BRD4 inhibitors, ARV-825 treatment results in a strikingly more pronounced effect on the levels of c-MYC, and downstream cell proliferation and apoptosis induction in BL (Burkitt’s Lymphoma) cell lines[1]. The IC50s of ARV-825 for all tested cell lines and primary AML cells at 72 hours are in the low nanomolar range (2-50 nM). ARV-825 treatment reduces PIM1 levels and phosphorylation of CXCR4 in AML cells while overexpression of PIM1 or Myc reverses the phenomena[3]. |
in vivo | In a mouse model of human leukemia, the leukemia burdens are significantly lower in the ARV-825 treated mice as confirmed by luciferase imaging, flow cytometry, spleen size and survived longer compared to control mice[3]. |
細胞アッセイ | 細胞株 | RS4;11 cells |
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濃度 | 3, 10, 30 nM | |
反応時間 | 3 h | |
実験の流れ | RS4;11 cells are treated for 3 h with each individual compound at indicated concentrations, and proteins are probed by specific antibodies. |
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動物実験 | 動物モデル | NOD/SCID gamma mice |
投薬量 | 5 mg/kg | |
投与方法 | i.p. |
Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] | PubMed: 38262581 |
Pharmacological inhibition of bromodomain and extra-terminal proteins induces an NRF-2-mediated antiviral state that is subverted by SARS-CoV-2 infection [ PLoS Pathog, 2023, 19(9):e1011657] | PubMed: 37747932 |
FET fusion oncoproteins interact with BRD4 and SWI/SNF chromatin remodelling complex subtypes in sarcoma [ Mol Oncol, 2022, 10.1002/1878-0261.13195] | PubMed: 35182012 |
Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection [ Microbiol Spectr, 2022, 10(4):e0241921] | PubMed: 35758684 |
Protein Ligand Interactions Using Surface Plasmon Resonance [ Methods Mol Biol, 2021, 2365:3-20] | PubMed: 34432236 |
Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer. [ J Exp Clin Cancer Res, 2019, 38(1):383] | PubMed: 31470872 |
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。