Biological Activity
Potent and selective extracellular signal-related kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852 nM for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). Potently blocks proliferation of HT29 cells (IC50 = 48 nM). Orally bioavailable.
Technical Data
M. Wt | 500.35 |
Formula | C24H20Cl2FN5O2 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 896720-20-0 |
PubChem ID | 11634725 |
InChI Key | WUTVMXLIGHTZJC-OAQYLSRUSA-N |
Smiles | O=C(N[C@H](CO)C3=CC(Cl)=CC=C3)C1=CC(C2=NC(NC4=CC=C(F)C=C4Cl)=NC=C2C)=CN1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 50.03 | 100 | |
ethanol | 12.51 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 500.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2 mL | 9.99 mL | 19.99 mL |
5 mM | 0.4 mL | 2 mL | 4 mL |
10 mM | 0.2 mL | 1 mL | 2 mL |
50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Aronov et al (2009) Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-related kinase (ERK) using conformational control. J.Med.Chem. 52 6362 PMID: 19827834
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