ABT-100
Names
Biological Activity
[Description]:
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].
[Related Catalog]:
[Target]
Farnesyltransferase[1]
[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[1]. Cell Proliferation Assay[1] 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.
[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[1]. Animal Model: C.B-17 scid male mice with EJ-1 cells[1] 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.
[References]
Chemical & Physical Properties
[ Density]:
1.29g/cm3
[ Boiling Point ]:
722ºC at 760 mmHg
[ Molecular Formula ]:
C27H19F3N4O3
[ Molecular Weight ]:
504.46000
[ Flash Point ]:
390.5ºC
[ Exact Mass ]:
504.14100
[ PSA ]:
104.09000
[ LogP ]:
5.04396
[ Index of Refraction ]:
1.589
[ Storage condition ]:
-20°C