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

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

Cat. No.: HY-112113 Purity: 98.53%
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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.

For research use only. We do not sell to patients.

SLV-2436 Chemical Structure

SLV-2436 Chemical Structure

CAS No. : 2095704-43-9

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 242 In-stock
Solution
10 mM * 1 mL in DMSO USD 242 In-stock
Solid
5 mg USD 220 In-stock
10 mg USD 350 In-stock
50 mg USD 1100 In-stock
100 mg USD 1600 In-stock
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Based on 1 publication(s) in Google Scholar

SLV-2436 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

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].

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

SLV-2436 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

350.80

Formula

C19H15ClN4O
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

O=C1C=CC(C2=CC3=C(C=C2)C(N)=NN3)=CN1CC4=CC=CC(Cl)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
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.
References

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
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SLV-2436 Related Classifications

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.

Keywords:

SLV-24362095704-43-9SEL201-88 SEL-201SLV2436SLV 2436SEL201SEL 201SEL-201MNKMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseInhibitorinhibitorinhibit

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