Kevetrin is an activator of p53.1,2 It increases levels of activated p53 and expression of p21 in A549 cells and decreases expression of the transcription factor E2F1 in a variety of cell lines.1,2 Kevetrin decreases cell viability in a panel of cancer cell lines with a mean IC50 value of 0.49 μM.3 It reduces tumor growth in MDA-MB-231, HT-29, PC3, HCT15, A549, NCI-H1975, CRL-1619, LNCaP, MIA PaCa, and SCC-5 mouse xenograft models when administered at a dose of 200 mg/kg.
1.Kumar, A., Hiran, T., Holden, S.A., et al.Abstract 4470: KevetrinTM, a novel small molecule, activates p53, enhances expression of p21, induces cell cycle arrest and apoptosis in a human cancer cell lineCancer Res.71(8 Supp)4470(2011) 2.Kumar, A., Holden, S.A., Chafai-Fadela, K., et al.Abstract 2874: Kevetrin targets both MDM2-p53 and Rb-E2F pathways in tumor suppressionCancer Res.72(8 Supp)2874(2012) 3.Menon, K.Nitrile derivatives and their pharmaceutical use and compositions(2012)