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ERK-IN-3 (ASN007 free base) is a potent and orally active inhibitor of ERK. It inhibits ERK1/2 with low single-digit nM IC50 values. It can be used for the research of cancers driven by RAS mutations.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $56 | In Stock | In Stock | |
| 5 mg | $126 | In Stock | In Stock | |
| 10 mg | $183 | In Stock | In Stock | |
| 25 mg | $297 | In Stock | In Stock | |
| 50 mg | $486 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $127 | In Stock | In Stock |
| Description | ERK-IN-3 (ASN007 free base) is a potent and orally active inhibitor of ERK. It inhibits ERK1/2 with low single-digit nM IC50 values. It can be used for the research of cancers driven by RAS mutations. |
| In vitro | ERK-IN-3 shows single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines.ERK-IN-3 inhibits the phosphorylation of ERK1/2 substrates like RSK1, FRA1, and Elk1 in various cell lines. |
| In vivo | ERK-IN-3 (daily p.o.) inhibits tumor growth in multiple BRAF and KRAS mutant xenograft models in mice that was well tolerated at efficacious doses. |
| Synonyms | ASN007 free base |
| Molecular Weight | 473.93 |
| Formula | C22H25ClFN7O2 |
| Cas No. | 2055597-12-9 |
| Smiles | Cc1cnc(NC2CCOCC2)nc1-n1cnc(c1)C(=O)N[C@H](CN)c1cc(F)cc(Cl)c1 |
| Relative Density. | 1.48 g/cm3 (Predicted) |
| Storage | store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 250 mg/mL (527.5 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.55 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
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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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