Nedometinib
Based on 1 publication(s) in Google Scholar
Nedometinib (NFX-179) is a specific MEK1 inhibitor with an IC50 of 135 nM. Nedometinib inhibits p-ERK, MAPK. Nedometinib exerts anticancer activity against squamous cell carcinoma. Nedometinib can be used for research in dermatosis, neurofibromatosis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.09%
- CAS 番号: 2252314-46-6
- 分子式: C17H16FIN4O3
- 分子量:470.24
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保管条件:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
MedChemExpress(MCE)の使用を引用している文献 Nedometinib
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生物活性
製品説明
IC50 & Target
[2]|
MEK1 135 nM (IC50) |
体外実験
NFX-179 shows cytotoxicity against HCT116 (KRAS-mutant) and A375 (BRAF-mutant) cell lines[2].
NFX-179 (0.01-30 μM; 72 h) inhibits the viability of human SCC cell lines IC1, SRB1, SRB12, and COLO16 in a dose-dependent manner, with IC50 values of 27 nM, 420 nM, 228 nM, and 91 nM respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
NFX-179 gel (0.01%-0.5%; topical application; 28 days) shows higher drug concentrations in the skin than in the plasma in minipigs, inhibiting the MAPK signaling pathway in the skin[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2252314-46-6
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性状 Solid
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分子量 470.24
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分子式 C17H16FIN4O3
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Color Off-white to light yellow
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SMILES
O=C(C1=C(NC2=CC=C(C=C2F)I)N(C)C3=C1C=CC=N3)NOCCO
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別名
NFX-179
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
Celastrol synergizes with MEK1 inhibitor nedometinib to overcome resistance in bladder cancer via dual suppression of CDK1/CDC5L and feedback-activated Akt/STAT3. [Abstract]2026 Mar:245:117629. PMID: 41386559
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (212.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1266 mL | 10.6329 mL | 21.2657 mL | 53.1643 mL |
| 5 mM | 0.4253 mL | 2.1266 mL | 4.2531 mL | 10.6329 mL | |
| 10 mM | 0.2127 mL | 1.0633 mL | 2.1266 mL | 5.3164 mL | |
| 15 mM | 0.1418 mL | 0.7089 mL | 1.4177 mL | 3.5443 mL | |
| 20 mM | 0.1063 mL | 0.5316 mL | 1.0633 mL | 2.6582 mL | |
| 25 mM | 0.0851 mL | 0.4253 mL | 0.8506 mL | 2.1266 mL | |
| 30 mM | 0.0709 mL | 0.3544 mL | 0.7089 mL | 1.7721 mL | |
| 40 mM | 0.0532 mL | 0.2658 mL | 0.5316 mL | 1.3291 mL | |
| 50 mM | 0.0425 mL | 0.2127 mL | 0.4253 mL | 1.0633 mL | |
| 60 mM | 0.0354 mL | 0.1772 mL | 0.3544 mL | 0.8861 mL | |
| 80 mM | 0.0266 mL | 0.1329 mL | 0.2658 mL | 0.6646 mL | |
| 100 mM | 0.0213 mL | 0.1063 mL | 0.2127 mL | 0.5316 mL |