ABT-100 is a potent, highly selective, and orally active inhibitor of farnesyl transferase [farnesyl-protein transferase] with broad-spectrum antitumor activity.

ABT-100 (0.1-100 nM; 7 days; EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells) treatment shows dose-dependent growth inhibition of human cancer cell lines. It also inhibits colony formation at concentrations comparable with which ABT-100 inhibits anchorage-dependent growth. 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 (6.25-12.5 mg/kg/day; subcutaneous injection; daily; for 21 days; C.B-17 scid male mice) treatment induces regression of EJ-1 tumors in mice.

Cell Line: EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells. Concentration: 0.1-100 nM. Incubation Time: 7 days

Animal Model: C.B-17 scid male mice with EJ-1 cells. Dosage: 6.25 mg/kg/day, 12.5 mg/kg/day. Administration: Subcutaneous injection; daily; for 21 days