ABT-100
| CAS No. | 450839-40-4 | Cat. No. | BCP42635 |
| Name | ABT-100 | ||
| Synonyms | ABT 100; ABT100; A367074; A 367074; A-367074; | ||
| Formula | C27H19F3N4O3 | M. Wt | 504.46 |
| Description | ABT-100 is an orally bioavailable farnesyltransferase inhibitor. ABT-100 inhibited proliferation of cells in vitro carrying oncogenic H-Ras (EJ-1 bladder; IC(50) 2.2 nmol/L), Ki-Ras (DLD-1 colon, MDA-MB-231 breast, HCT-116 colon, and MiaPaCa-2 pancreatic; IC(50) range, 3.8-9.2 nmol/L), and wild-type Ras (PC-3 and DU-145; IC(50), 70 and 818 nmol/L, respectively) as well as clonogenic potential. ABT-100 shows 70% to 80% oral bioavailability in mice. ABT-100 regressed EJ-1 tumors (2-12.5 mg/kg/d s.c., every day for 21 days) and showed significant efficacy in DLD-1, LX-1, MiaPaCa-2, or PC-3 tumor-bearing mice (6.25-50 mg/kg/d s.c. once daily or twice daily orally). | ||
| Pathways | Protease/Metabolic Enzyme | ||
| Targets | FTase | ||
Structure
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