ABT-100

ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity[1].

[1] Ferguson D, et al. Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, proapoptotic, and antiangiogenic effects in xenograft models. Clin Cancer Res. 2005 Apr 15;11(8):3045-54. DOI:10.1158/1078-0432.CCR-04-2041
[2] VINICIO CARLONI  Pietro P  Francesco Vizzutti. Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent.[J]. Clinical Cancer Research, 2005, 11 11: 4266-4274. DOI: 10.1158/1078-0432.ccr-04-2386
[3] LOREN G. FONG. A Protein Farnesyltransferase Inhibitor Ameliorates Disease in a Mouse Model of Progeria[J]. Science, 2006, 311 5767. DOI: 10.1126/science.1124875