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 | C26H27F4N7O2 |
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分子量 | 545.53 | CAS No. | 1375465-09-0 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (183.3 mM) | |
Ethanol | 29 mg/mL (53.15 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 | CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR. |
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in vitro | CNX-2006 is a novel irreversible EGFR tyrosine kinase inhibitor, specifically inhibits activating mutations of EGFR as well as the T790M mutation while having very weak inhibition at wild-type EGFR. In in vitro modeling of acquired resistance, continuous CNX-2006 treatment on drug-sensitive EGFR mutant cells leads to resistance more slowly than erlotinib. Dose escalation with CNX-2006 leads to differential effects in different lines, but does not select for T790M-mediated resistance. [1]CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.[2] |
in vivo | CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model. [1] [2] |
キナーゼアッセイ | Growth inhibition assays | |
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Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays. | ||
細胞アッセイ | 細胞株 | HEK293 |
濃度 | ~1000 nM | |
反応時間 | 6 h | |
実験の流れ | Cells with endogenous or transiently transfected mutant EGFRs (293 cells) are treated with inhibitors for 6 hours and then corresponding lysates are extracted and analyzed by immunoblotting. | |
動物実験 | 動物モデル | Nude mice |
投薬量 | 25 mg/kg | |
投与方法 | i.p. |
Data from [Data independently produced by , , Cancer Sci, 2016, 107:461-468.]
Extracellular vesicle drug occupancy enables real-time monitoring of targeted cancer therapy [ Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w] | PubMed: 33686255 |
Oncogene swap as a novel mechanism of acquired resistance to epidermal growth factor receptor-tyrosine kinase inhibitor in lung cancer. [Mizuuchi H, et al. Cancer Sci, 2016, 107(4):461-8] | PubMed: 26845230 |
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。