ABT-100是一种有效的，高选择性和口服活性的farnesyltransferase抑制剂。ABT-100抑制细胞增殖(对于EJ-1，DLD-1，MDA-MB-231，HCT-116，MiaPaCa-2，PC-3和DU-145细胞的IC50分别为2.2nM，3.8nM，5.9nM，6.9nM，9.2nM，70nM和818nM)，可增加细胞凋亡并减少血管生成。ABT-100具有广谱抗肿瘤活性。
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].
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[1]. Cell Proliferation Assay[1] Cell Line: EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells
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[1]. Animal Model: C.B-17 scid male mice with EJ-1 cells[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.
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