PF-04880594

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Chemical Information

Product name：PF-04880594	Purity：99% min
CAS NO：1111636-35-1	Solubility：
Molecular Formula：C₁₉H₁₆F₂N₈	Package：Package according to customer requirements
Molecular Weight：394.381	Storage：Store at -20℃

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Remarks

PF-04880594 is a RAF inhibitor, which induces ERK phosphorylation and RAF dimerization in those epithelial tissues that undergo hyperplasia. PF-04880594 stimulates production of the inflammatory cytokine interleukin 8 in HL-60 cells. Epithelial tissue hyperplasia induced by the RAF inhibitor PF-04880594 is attenuated by a clinically well-tolerated dose of the MEK inhibitor PD-0325901. The combination treatment with PF-04880594 and MEK inhibitors might greatly increase the safety and therapeutic index of RAF inhibitors for the treatment of melanoma and other cancers.

References

1: Torti VR, Wojciechowicz D, Hu W, John-Baptiste A, Evering W, Troche G, Marroquin LD, Smeal T, Yamazaki S, Palmer CL, Burns-Naas LA, Bagrodia S. Epithelial tissue hyperplasia induced by the RAF inhibitor PF-04880594 is attenuated by a clinically well-tolerated dose of the mek inhibitor PD-0325901. Mol Cancer Ther. 2012 Oct;11(10):2274-83. doi: 10.1158/1535-7163.MCT-11-0984. Epub 2012 Jul 2. PubMed PMID: 22752429.

2: Lee NV, Lira ME, Pavlicek A, Ye J, Buckman D, Bagrodia S, Srinivasa SP, Zhao Y, Aparicio S, Rejto PA, Christensen JG, Ching KA. A novel SND1-BRAF fusion confers resistance to c-Met inhibitor PF-04217903 in GTL16 cells though MAPK activation. PLoS One. 2012;7(6):e39653. doi: 10.1371/journal.pone.0039653. Epub 2012 Jun 22. PubMed PMID: 22745804; PubMed Central PMCID: PMC3382171.