Biological Activity
Selective MEK inhibitor (Ki = 300 nM in vitro). Suppresses FGF-mediated angiogenesis in vivo and decreases VEGF expression. Enhances the therapeutic efficacy of taxol (Cat. No. 1097) in vivo. Orally active.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 478.66 |
| Formula | C17H14ClF2IN2O2 |
| Storage | Store at +4°C |
| CAS Number | 212631-79-3 |
| PubChem ID | 6918454 |
| InChI Key | GFMMXOIFOQCCGU-UHFFFAOYSA-N |
| Smiles | FC1=C(NC2=CC=C(I)C=C2Cl)C(C(NOCC3CC3)=O)=CC=C1F |
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 | 47.87 | 100 | |
| ethanol | 11.97 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 478.66. 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 | 2.09 mL | 10.45 mL | 20.89 mL |
| 5 mM | 0.42 mL | 2.09 mL | 4.18 mL |
| 10 mM | 0.21 mL | 1.04 mL | 2.09 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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References
References are publications that support the products' biological activity.
Allen et al (2003) CI-1040 (PD184252), a targeted signal transduction inhibitor of MEK (MAPKK). Semin.Oncol. 30 105 PMID: 14613031
McDaid et al (2005) Enhancement of the therapeutic efficacy of taxol by the mitogen-activated protein kinase kinase inhibitor CI-1040 in nude mice bearing human heterotransplants. Cancer Res. 65 2854 PMID: 15805287
Solit et al (2006) BRAF mutation predicts sensitivity to MEK inhibition. Nature 439 358 PMID: 16273091
Keywords: PD 184352, supplier, pfizer, mek1, mek2, mkk1, mkk2, inhibitors, inhibits, selective, mapk, signaling, signalling, map, kinases, PD184352, CI1040, CI-1040, MEK, MEK, Tocris Bioscience
