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PD 0325901Cat. No. 4192 |
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Alternative Name: PD325901 Chemical Name: N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide |
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. Orally active.Licensing Information
Sold for research purposes under agreement from Pfizer Inc.Certificate of Analysis / Safety Data Sheet
References
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.
Barrett et al (2008) The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg.Med.Chem.Lett. 18 6501. PMID: 18952427.
Friday and Adjei (2008) Advances in targeting the Ras/Raf/MEK/Erk mitogen-activated protein kinase cascade with MEK inhibitors for cancer therapy. Clin.Cancer Res. 14 342. PMID: 18223206.
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.
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Keywords: PD 0325901, supplier, pfizer, PD0325901, PD325901, mek1, mek2, mkk1, mkk2, mapk, signalling, signaling, selective, inhibitors, proapoptotic
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