Biological Activity
Highly potent and selective p38α inhibitor (IC50 = 10 nM). Also blocks TNFα production in LPS-stimulated HWB in vitro (IC50 = 177 nM). Displays 1000-fold selectivity over closely related kinases, including ERK1, MK2 and JNK1-3.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of VX 745 is reviewed on the chemical probes website.
Technical Data
| M. Wt | 436.26 |
| Formula | C19H9Cl2F2N3OS |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 209410-46-8 |
| PubChem ID | 3038525 |
| InChI Key | VEPKQEUBKLEPRA-UHFFFAOYSA-N |
| Smiles | O=C2N=CN1N=C(SC4=CC=C(F)C=C4F)C=CC1=C2C3=C(Cl)C=CC=C3Cl |
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 | 43.63 | 100 | |
| ethanol | 2.18 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 436.26. 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 | 2.29 mL | 11.46 mL | 22.92 mL |
| 5 mM | 0.46 mL | 2.29 mL | 4.58 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.29 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Bagley et al (2007) Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells. Bioorg.Med.Chem.Lett. 17 5107 PMID: 17659871
Goldstein et al (2010) Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J.Med.Chem. 53 2345 PMID: 19950901
Duffy et al (2011) The discovery of VX-745: a novel and selective p38α kinase inhibitor. ACS Med.Chem.Lett. 2 758 PMID:
Keywords: VX 745, supplier, VX745, p38a, p38alpha, p38α, MAPK, inhibitors, inhibits, selective, potent, p38, p38, Tocris Bioscience
