SLV-2436 (SEL201-88)
SEL-201 (SLV-2436, SEL201-88) is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50 of 10.8 ?nM and 5.4 nM, respectively.
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包装价格促销价数量
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5mg￥2012.001610.00- +
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10mg￥3262.002610.00- +
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50mg￥10475.008380.00- +
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100mg￥14362.0011490.00- +
- 货号: ajce50116
- CAS: 2095704-43-9
- 别名: SEL201-88; SEL-201
- 分子式: C19H15ClN4O
- 分子量: 350.8
- 纯度: ＞98%
- 溶解度: DMSO : ≥ 100 mg/mL (285.06 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
SEL-201 (SLV-2436, SEL201-88) is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50 of 10.8 ?nM and 5.4 nM, respectively.
[1] Yao Zhan, et al. J Clin Invest. 2017 Nov 1;127(11):4179-4192.
Protocol
Cell experiment: | 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]. |
Animal experiment: | 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]. |
参考文献: [1]. Zhan Y, et al. MNK1/2 inhibition limits oncogenicity and metastasis of KIT-mutant melanoma. J Clin Invest. 2017 Nov 1;127(11):4179-4192. | |
