Synonyms: (S)-1-Benzyl-2-(4-(2-(2-phenyl-1H-benzo[d]imidazol-1-yl)-2-(piperidin-4-yl)ethoxy)phenyl)-1H-benzo[d]imidazole trihydrochloride; 2-[4-[(2S)-2-(2-Phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole trihydrochloride
Molecular Formula: C40H37N5O · 3HCl
Molecular Weight: 713.14
Linear Structural Formula: C40H37N5O · 3HCl
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: Deltarasin is a membrane-permeable benzimidazole derivative that effectively abolishes cellular KRas plasma membrane localization (5 muM for 1 hr) by blocking KRas-PDEdelta interaction via high affinity interaction with PDEdelta prenyl-binding pocket (KD = 38 nM). Deltarasin inhibits oncogenic KRas-dependent proliferation (by ~50% of Panc-Tu-I cells; 5muM for 70 hrs) and survival (52% and 46% death induction of Panc-Tu-I and Capan-1 cells, respectively; 5muM for 24 hrs) in human pancreatic ductal adenocarcinoma (PDAC) cultures and is efficacious against Panc-Tu-I xenograft-derived tumor growth in mice in vivo (60% and 80% retardation on day 9, respectively, with 15 mg/kg q.d. or 10 mg/kg b.i.d. via i.p.).