1. MAPK/ERK Pathway
  2. MNK

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

Cat. No.: HY-112113 Purity: 98.13%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 242 In-stock
Estimated Time of Arrival: December 31
5 mg USD 220 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1100 In-stock
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100 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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[1]

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].

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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (285.06 mM)

*"≥" 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
10 mM 0.2851 mL 1.4253 mL 2.8506 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

350.80

Formula

C₁₉H₁₅ClN₄O

CAS No.

2095704-43-9

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SLV-2436
Cat. No.:
HY-112113
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SLV-2436

Cat. No.: HY-112113