Biological Activity
Potent MEK1 and MEK2 inhibitor. Inhibits MEK activity in mouse colon 26 cells (IC50 = 0.33 nM). Inhibits the growth of melanoma cell lines in vitro and in vivo; induces G1-phase cell cycle arrest and apoptosis in a mouse xenograft model. Also inhibits production of proangiogenic cytokines such as VEGF. Enhances generation of induced pluripotent stem cells (iPSCs). Orally active.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries
PD 0325901 is also offered as part of the Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 482.19 |
| Formula | C16H14F3IN2O4 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 391210-10-9 |
| PubChem ID | 9826528 |
| InChI Key | SUDAHWBOROXANE-SECBINFHSA-N |
| Smiles | FC1=CC(I)=CC=C1NC2=C(C(NOC[C@H](O)CO)=O)C=CC(F)=C2F |
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 | 12.05 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 482.19. 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 | 2.07 mL | 10.37 mL | 20.74 mL |
| 5 mM | 0.41 mL | 2.07 mL | 4.15 mL |
| 10 mM | 0.21 mL | 1.04 mL | 2.07 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.41 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Barrett et al (2008) The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg.Med.Chem.Lett. 18 6501 PMID: 18952427
Ciuffreda et al (2009) Growth-inhibitor and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations. Neoplasia 11 720 PMID: 19649202
Sebolt-Leopold et al (2004) The biological profile of PD 0325901: a second generation analog of CI-1040 with improved pharmaceutical potential. Proc.Amer.Assoc.Cancer Res. 45 925 PMID:
Lin et al (2009) A chemical platform for improved induction of human iPSCs. Nat.Methods. 6 805 PMID: 19838168
Keywords: PD 0325901, supplier, pfizer, PD0325901, PD325901, mek1, mek2, mkk1, mkk2, mapk, signalling, signaling, selective, inhibitors, inhibits, proapoptotic, organoids, PD325901, MEK, Reprogramming, MEK, Tocris Bioscience
