Description
A potent FTase inhibitor (IC50 = 1.3 nM); selective for FTase over GGTase (IC50 = 1,900 nM); inhibits the growth of MEK2, A2780, and PC3 cancer cells expressing wild-type Ras (IC50s = 2.5, 0.04, and 0.15 μM, respectively), as well as HCT116, MIP, RC-165, and MIA PaCa-2 cells expressing mutant K-Ras (IC50s = 0.06, 0.3, 0.3, and 0.12 μM, respectively); induces apoptosis in HCT116 cells; curative in an HCT116 mouse xenograft model at 600 mg/kg; reduces tumor growth in Calu-1, HT-29, EJ-1, and MIA PaCa-2 mouse xenograft models
Formal name: (3R)-2,3,4,5-tetrahydro-1-(1H-imidazol-5-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile
Synonyms:
Molecular weight: 489.6
CAS: 195987-41-8
Purity: ≥98%
Formulation: A solid
