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.
体外研究
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.
Cell Proliferation Assay
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
Result:
Demonstrated dose-dependent growth inhibition of human cancer cell lines.
体内研究
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.
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.
分子式
C27H19F3N4O3
分子量
504.46
CAS号
450839-40-4
运输条件
Room temperature in continental US; may vary elsewhere.