1. MAPK/ERK Pathway
  2. MNK
  3. SLV-2436

SLV-2436  (Synonyms: SEL201-88; SEL-201)

目录号: HY-112113 纯度: 98.53%
COA 产品使用指南

SLV-2436 是一种高效且 ATP 竞争性的 MNK1MNK2 抑制剂,IC50 分别为 10.8 nM 和 5.4 nM。

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SLV-2436 Chemical Structure

SLV-2436 Chemical Structure

CAS No. : 2095704-43-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2035
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1 mg ¥740
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5 mg ¥1850
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10 mg ¥3000
In-stock
50 mg ¥9700
In-stock
100 mg
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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

IC50 & Target

MNK2

5.4 nM (IC50)

MNK1

10.8 nM (IC50)

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

To investigate the pharmacodynamic properties of SLV-2436 (SEL201), 5 consecutive oral doses of 10, 25, and 50 mg/kg are administered to mice every 12 hours (twice-daily schedule). At the 10 mg/kg twice-daily dosage, 4 hours after the fifth administration, a low plasma concentration of 125 ng/mL SLV-2436 is determined. However, dosing at 25 and 50 mg/kg twice daily, equivalent to 50 and 100 mg/kg/d of SLV-2436, yields 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, SLV-2436 is 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 SLV-2436 at the dosage of 50 mg/kg twice daily, that is, 100 mg/kg/d, for 37 days is well tolerated in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

350.80

Formula

C19H15ClN4O

CAS 号
性状

固体

颜色

Light brown to brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (285.06 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8506 mL 14.2531 mL 28.5063 mL
5 mM 0.5701 mL 2.8506 mL 5.7013 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

SLV-2436 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 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
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
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
SLV-2436
目录号:
HY-112113
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