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SLV-2436

产品编号 T4424 CAS 2095704-43-9

别名: SEL-201, SLV 2436, SEL201-88

SLV-2436 (SEL201-88) 是一种高效且 ATP 竞争性的MNK1和MNK2抑制剂，IC50分别为 10.8 和 5.4 nM。

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SLV-2436, CAS 2095704-43-9

规格	价格/CNY	货期
1 mg	￥ 611	现货
2 mg	￥ 886	现货
5 mg	￥ 1,460	现货
10 mg	￥ 2,390	现货
25 mg	￥ 3,970	现货
50 mg	￥ 5,780	现货
100 mg	￥ 7,880	现货
1 mL * 10 mM (in DMSO)	￥ 1,580	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	SLV-2436 (SEL201-88) is a novel effective and ATP-competitive inhibitor of MNK1 and MNK2 (IC50: 10.8/5.4 nM).
靶点活性	MNK1:10.8 nM, MNK2:5.4 nM
体外活性	In vitro kinase assays, using recombinant MNK1 and MNK2 protein and increasing concentrations of the SEL201 show that SEL201 is highly potent, with an IC50 of 10.8 ?nM and 5.4 ?nM for MNK1 and MNK2, respectively. To confirm the kinome selectivity of SEL201, the broad KINOMEscan (DiscoverX) competitive binding assay at 1 μM is performed, which included 450 distinct kinases (32). The binding profile for SEL201 is observed, which was significantly concentrated in the CAMK family of kinases that comprises MNK1 and MNK2.
体内活性	To investigate the pharmacodynamic properties of SEL201, 5 consecutive oral doses of 10, 25, and 50 mg/kg were administered to mice every 12 hours (twice-daily schedule). At the 10 mg/kg twice-daily dosage, 4 hours after the fifth administration, we determined a low plasma concentration of 125 ng/ml SEL201. However, dosing at 25 and 50 mg/kg twice daily, equivalent to 50 and 100 mg/kg/d of SEL201, yielded substantially increased dose-dependent plasma exposure, reaching an average level of 1,299 ng/ml and 2,075 ng/ml, respectively. At the 24-hour time point, SEL201 was still detectable in the plasma, with dose-dependent concentrations of 9, 73, and 124 ng/ml in the 10, 25, and 50 mg/kg twice-daily treatment groups. Oral (p.o.) administration of SEL201 at the dosage of 50 mg/kg twice daily, that is, 100 mg/kg/d, for 37 days was well tolerated in mice. Furthermore, 37 days of consecutive administration of SEL201, at the dosage of 100 mg/kg/d, did not result in any overt clinical signs of toxicity. A blood chemistry panel was performed, including hematological and biochemical parameters, at the study endpoint and confirmed that multiple dosings with SEL201 at 100 mg/kg/d is safe. Nevertheless, SEL201 showed very good oral bioavailability, with a maximum plasma concentration of 1,078 ng/ml reached 0.25 hours after p.o. administration.
细胞实验	Western blot analysis. Cells were treated with dasatinib, imatinib, or SEL201 at the indicated times, and pellets were harvested to obtain protein extracts. Briefly, cell pellets were lysed in RIPA buffer (50 mM Tris-HCl, pH 8.0, with 150 mM sodium chloride, 1.0% Igepal CA-630 [NP-40], 0.5% sodium deoxycholate, and 0.1% SDS). After sonication, cell lysates were centrifuged at 15,871 g for 15 minutes. The supernatants were collected, and protein concentrations were quantified. Equal amounts of protein were loaded and separated on a 10% SDS-PAGE. After transferring to a nitrocellulose membrane (Bio-Rad), 5% milk/TBS was used to block for 1 hour, and then probed for target antibodies overnight at 4°C. After incubation with HRP-conjugated secondary antibodies for 1 hour at room temperature, the signals of targeted protein were developed with chemiluminescence substrate ECL Western blotting detection reagent.
动物实验	All animals were handled in strict accordance with the good animal practice and maintained according to the standards of pathogen-free conditions. The pharmacokinetic profile of SEL201 was assessed in 6-week-old female CD-1 mice (3 animals per time point). SEL201 was freshly dissolved in DMSO and then diluted in Captisol (Ligand) 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 were sacrificed at 8 time points (5, 15, and 30 minutes and 1, 2, 4, 6, and 24 hours) and blood samples harvested. Plasma samples were collected and stored at –80°C for further analysis. To evaluate the pharmacodynamic properties of SEL201, 10- to 16-week-old male C57BL/6 mice (stock 000664, The Jackson Laboratory) were divided into a control group and 3 dosing groups. Animals were given either vehicle (DMSO + N,N-Dimethylacetamide + Captisol) or SEL201 at 10-, 25-, and 50-mg/kg doses (freshly dissolved). Drugs were administered p.o. in a volume of 10 μl per 1 g of body weight. Each animal received a total of 5 doses with the twice-daily schedule (i.e., every 12 hours). Body weight was 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 were collected and stored at –80°C for further analysis. For safety assessment of SEL201, 7- to 8-week-old tumor-bearing female Hsd: Athymic Nude-Foxn1nu mice (strain code 069, Envigo) were used. Before use, SEL201 was freshly dissolved, and doses of 50 mg/kg were administered twice daily p.o. in a volume of 10 μl per 1 g of body weight. Body weight was assessed every day. At the end of the experiment on day 37, mice were anesthetized and blood samples for total cell counts and biochemistry were obtained.

别名	SEL-201, SLV 2436, SEL201-88
分子量	350.8
分子式	C19H15ClN4O
CAS No.	2095704-43-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (142.53 mM)

溶液配制表

可选溶剂	浓度体积质量	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
	20 mM	0.1425 mL	0.7127 mL	1.4253 mL	3.5633 mL
	50 mM	0.057 mL	0.2851 mL	0.5701 mL	1.4253 mL
	100 mM	0.0285 mL	0.1425 mL	0.2851 mL	0.7127 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Zhan Y, Guo J, Yang W, et al. MNK1/2 inhibition limits oncogenicity and metastasis of KIT-mutant melanoma.[J]. Journal of Clinical Investigation, 2017, 127(11):4179.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

SLV-2436 2095704-43-9 MAPK MNK MAP kinase interacting kinase inhibit SEL-201 SLV 2436 SEL201 MAPK interacting kinase Mitogen activated protein kinase interacting kinase Inhibitor SEL 201 SEL201-88 SLV2436 inhibitor

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SLV-2436

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords