SLV-2436
Based on 1 Customer Validation
SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 nM and 5.4 nM, respectively.
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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: 98.03%
- CAS 番号: 2095704-43-9
- 分子式: C19H15ClN4O
- 分子量:350.80
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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MNK2 5.4 nM (IC50) |
MNK1 10.8 nM (IC50) |
To confirm the kinome selectivity of SLV-2436 (SEL201), the broad KINOMEscan competitive binding assay is performed at 1 μM, which includes 450 distinct kinases. The observed binding profile for SLV-2436 is significantly concentrated in the CAMK family of kinases that comprises MNK1 and MNK2. SLV-2436-treated KIT-mutant melanoma cells have lower oncogenicity and reduced metastatic ability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2095704-43-9
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性状 Solid
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分子量 350.80
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分子式 C19H15ClN4O
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Color Light brown to brown
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SMILES
O=C1C=CC(C2=CC3=C(C=C2)C(N)=NN3)=CN1CC4=CC=CC(Cl)=C4
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別名
SEL201-88; SEL-201
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (285.06 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. 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. 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
One thousand HBL, MM61, MM111, and M230 cell lines per well are seeded in 6-well plates, and the cells are allowed to adhere overnight. After overnight incubation, the cells are treated with either DMSO (control) or SLV-2436 (5 μM). After 14 days, media are removed from the wells, and the cells are stained with 0.5% (wt/vol) crystal violet in 70% ethanol. After 1 hour of incubation at room temperature, staining dye is washed, and the colony numbers are counted by GelCount. The experiment is done in triplicate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
The pharmacokinetic profile of SLV-2436 is assessed in 6-week-old female CD-1 mice. SLV-2436 is freshly dissolved in DMSO and then diluted in Captisol for administration with a volume of 10 μL per 1 g of body weight via the oral (p.o.; 5 mg/kg) or i.v. (2 mg/kg) route. Animals are sacrificed at 8 time points (5, 15, and 30 minutes and 1, 2, 4, 6, and 24 hours) and blood samples harvested. Plasma samples are collected and stored at -80°C for further analysis. To evaluate the pharmacodynamic properties of SLV-2436, 10- to 16-week-old male C57BL/6 mice are divided into a control group and 3 dosing groups. Animals are given either vehicle (DMSO+N,N-Dimethylacetamide+Captisol) or SLV-2436 at 10-, 25-, and 50-mg/kg doses (freshly dissolved). Drugs are administered p.o. in a volume of 10 μL per 1 g of body weight. Each animal receive a total of 5 doses with twice-daily schedule (i.e., every 12 hours). Body weight is assessed once daily. Six animals per experimental group supported sample collection at 2 time points (i.e., 4 hours and 24 hours) after the last, fifth administration, with 3 animals per time point. Plasma samples are collected and stored at -80°C for further analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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. 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 | 2.8506 mL | 14.2531 mL | 28.5063 mL | 71.2657 mL |
| 5 mM | 0.5701 mL | 2.8506 mL | 5.7013 mL | 14.2531 mL | |
| 10 mM | 0.2851 mL | 1.4253 mL | 2.8506 mL | 7.1266 mL | |
| 15 mM | 0.1900 mL | 0.9502 mL | 1.9004 mL | 4.7510 mL | |
| 20 mM | 0.1425 mL | 0.7127 mL | 1.4253 mL | 3.5633 mL | |
| 25 mM | 0.1140 mL | 0.5701 mL | 1.1403 mL | 2.8506 mL | |
| 30 mM | 0.0950 mL | 0.4751 mL | 0.9502 mL | 2.3755 mL | |
| 40 mM | 0.0713 mL | 0.3563 mL | 0.7127 mL | 1.7816 mL | |
| 50 mM | 0.0570 mL | 0.2851 mL | 0.5701 mL | 1.4253 mL | |
| 60 mM | 0.0475 mL | 0.2376 mL | 0.4751 mL | 1.1878 mL | |
| 80 mM | 0.0356 mL | 0.1782 mL | 0.3563 mL | 0.8908 mL | |
| 100 mM | 0.0285 mL | 0.1425 mL | 0.2851 mL | 0.7127 mL |