Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 8,000 | |||
2 mg | 在庫あり | ¥ 11,000 | |||
5 mg | 在庫あり | ¥ 17,500 | |||
10 mg | 在庫あり | ¥ 29,500 | |||
25 mg | 在庫あり | ¥ 54,000 | |||
50 mg | 在庫あり | ¥ 97,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 21,500 |
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. |
ターゲット&IC50 | EGFR (mutant):<20 nM |
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] |
キナーゼ試験 | Growth inhibition assays: Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays. |
細胞研究 | 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.(Only for Reference) |
動物実験 | Animal Models: Nude miceFormulation: 5% DMSO:15% Solutol HS15 in PBSDosages: 25 mg/kgAdministration: i.p. |
別名 | CNX 2006, CNX2006 |
分子量 | 545.53 |
分子式 | C26H27F4N7O2 |
CAS No. | 1375465-09-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMF: soluble
DMSO: 91 mg/mL(166.8 mM)
You can also refer to dose conversion for different animals. 詳細
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CNX-2006 1375465-09-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR CNX 2006 HER1 inhibit Epidermal growth factor receptor ErbB-1 CNX2006 Inhibitor inhibitor