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ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50 values of 0.82 μM for ERK5 and 3 μM for ERK5 (MEF2D).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $41 | In Stock | In Stock | |
| 5 mg | $97 | In Stock | In Stock | |
| 10 mg | $172 | In Stock | In Stock | |
| 25 mg | $297 | In Stock | In Stock | |
| 50 mg | $446 | In Stock | In Stock | |
| 100 mg | $645 | In Stock | In Stock | |
| 200 mg | $887 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $108 | In Stock | In Stock |
| Description | ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50 values of 0.82 μM for ERK5 and 3 μM for ERK5 (MEF2D). |
| Targets&IC50 | ERK5:0.82 μM, ERK5 MEF2D:3 μM |
| In vivo | ERK5-IN-2 (compound 46) (p.o.; 100?mg/kg; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days) has an anti-angiogenic effect and low concentrations of haemoglobin.ERK5-IN-2 (i.v. or p.o.; 10?mg/kg for 0.083-24?hours) exhibits low intrinsic clearance and has high flux and a low efflux ratio (ER) in a caco-2?cell permeability assay in both human and mouse. |
| Molecular Weight | 388.19 |
| Formula | C17H11BrFN3O2 |
| Cas No. | 1888305-96-1 |
| Smiles | Fc1cccc(Br)c1C(=O)c1c[nH]c(c1)C(=O)Nc1cccnc1 |
| Relative Density. | 1.628 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 10 mg/mL (25.76 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.58 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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