ABT-100

ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation ( IC 50 s 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 In Vitro 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. Also inhibits colony formation at concentrations comparable with which ABT-100 inhibits anchorage-dependent growth. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 Result: Demonstrated dose-dependent growth inhibition of human cancer cell lines. In Vivo ABT-100 (6.25-12.5 mg/kg/day; subcutaneous injection; daily; for 21 days; C.B-17 scid male mice) treatment regresses EJ-1 tumors in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 Result: Regressed EJ-1 tumors in C.B-17 scid male mice. Form:Solid IC50& Target:Farnesyltransferase

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