受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H24Cl2N4O4 |
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分子量 | 503.38 | CAS No. | 1707289-21-1 | ||||||||
Solubility (25°C)* | 体外 | DMSO (warmed with 50ºC water bath) | 100 mg/mL (198.65 mM) | ||||||||
Ethanol (warmed with 50ºC water bath) | 2 mg/mL (3.97 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 | Fisogatinib (BLU-554) is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM. |
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in vitro | BLU-554 exploits a unique interaction with FGFR4 to confer potency and selectivity |
in vivo | BLU-554 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models[1]. |
細胞アッセイ | 細胞株 | ST8814 resistant cells |
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濃度 | 1 µM | |
反応時間 | 4 h | |
実験の流れ | ST8814 resistant cells were treated with DMSO or BLU-554 at 1 µM for 4 hrs. |
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動物実験 | 動物モデル | Male FVB/NRj mice |
投薬量 | 10 mg/kg | |
投与方法 | p.o. |
FGF19-Induced Inflammatory CAF Promoted Neutrophil Extracellular Trap Formation in the Liver Metastasis of Colorectal Cancer [ Adv Sci (Weinh), 2023, 10(24):e2302613] | PubMed: 37345586 |
Fibroblast growth factor receptor 4 promotes glioblastoma progression: a central role of integrin-mediated cell invasiveness [ Acta Neuropathol Commun, 2022, 10(1):65] | PubMed: 35484633 |
BLU-554, A selective inhibitor of FGFR4, exhibits anti-tumour activity against gastric cancer in vitro [ Biochem Biophys Res Commun, 2022, 595:22-27] | PubMed: 35093636 |
EGFR activation limits the response of liver cancer to lenvatinib [ Nature, 2021, 595(7869):730-734] | PubMed: 34290403 |
Activation of receptor tyrosine kinases mediates acquired resistance to MEK inhibition in malignant peripheral nerve sheath tumors [ Cancer Res, 2020, canres.1992.2020] | PubMed: 33203698 |
Chemosensitivity of Patient-Derived Cancer Stem Cells Identifies Colorectal Cancer Patients with Potential Benefit from FGFR Inhibitor Therapy [ Cancers (Basel), 2020, 12(8):E2010] | PubMed: 32708005 |
Protein tyrosine kinase 2: a novel therapeutic target to overcome acquired EGFR-TKI resistance in non-small cell lung cancer [ Respir Res, 2019, 20(1-:270] | PubMed: 31791326 |
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。