[CAS NO. 2095704-43-9] SLV-2436
PRODUCTS SPECIFICATIONS [2095704-43-9]
DESCRIPTION [2095704-43-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 350.80 |
| Molecular Formula | C19H15ClN4O |
| SMILES | O=C1C=CC(C2=CC3=C(C=C2)C(N)=NN3)=CN1CC4=CC=CC(Cl)=C4 |
Summary
IC50 & Target
|
MNK2 5.4 nM (IC 50 ) |
MNK1 10.8 nM (IC 50 ) |
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.
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.
Appearance
Solid
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
DMSO : ≥ 100 mg/mL ( 285.06 mM )
* "≥" means soluble, but saturation unknown.
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 |