WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406212
Description: 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.
MedKoo Cat#: 406212
Chemical Formula: C19H16F2N8
Exact Mass: 394.1466
Molecular Weight: 394.38
Elemental Analysis: C, 57.86; H, 4.09; F, 9.63; N, 28.41
Synonym: PF04880594; PF-04880594; PF 04880594.
IUPAC/Chemical Name: 3-((4-(1-(2,2-difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propanenitrile
SMILES Code: N#CCCNC1=NC=CC(C2=CN(CC(F)F)N=C2C3=CN=C(NC=C4)C4=C3)=N1
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.