Description
PD-325901 is an anticancer chemotherapeutic MEK1/2 and Raf inhibitor that is particularly effective against cancers harboring B-Raf or Ras mutations such as V600E. PD-325901 decreases levels of phosphorylated ERK1/2, cyclin D1, and thymidine kinase 1. PD-325901 also induces cell cycle arrest at the G0/G1 phase, inhibiting proliferation in thyroid cancer cell lines. In vivo, this compound decreases tumor growth and size. Additionally, PD-325901 displays antiviral benefit, synergizing with other treatments in cellular models of influenza infection.
References
Haasbach E, Hartmayer C, Planz O. Combination of MEK inhibitors and oseltamivir leads to synergistic antiviral effects after influenza A virus infection in vitro. Antiviral Res. 2013 May;98(2):319-24. PMID: 23523553.
Leyton J, Smith G, Lees M, et al. Noninvasive imaging of cell proliferation following mitogenic extracellular kinase inhibition by PD0325901. Mol Cancer Ther. 2008 Sep;7(9):3112-21. PMID: 18790789.
Liu D, Xing M. Potent inhibition of thyroid cancer cells by the MEK inhibitor PD0325901 and its potentiation by suppression of the PI3K and NF-kappaB pathways. Thyroid. 2008 Aug;18(8):853-64. PMID: 18651802.
Brown AP, Carlson TC, Loi CM, et al. Pharmacodynamic and toxicokinetic evaluation of the novel MEK inhibitor, PD0325901, in the rat following oral and intravenous administration. Cancer Chemother Pharmacol. 2007 Apr;59(5):671-9. PMID: 16944149.