RGNCY-0087 (3144 Pan-Ras inhibitor)
3144 is a multivalent PAN-RAS inhibitor shown to bind to RAS proteins. 3144 exhibited lethality in cell lines partially dependent on RAS protein expression by inducing caspase activity to a similar level as another apoptosis inducer, staurosporine. It is metabolically stable in liver microsomes and has anti-tumor activity in xenograft mouse cancer models (MDA-MB-231 and PDTALL22 patient T-ALL sample) when administered orally or intravenously. At high concentrations, 3144 demonstrated toxicity and off-target activity in vitro and in vivo. 3144 is an effective tool in developing pan-RAS inhibitory treatments for cancers.
Systematic Name: 3-amino-N-(3-(5-((4-(2,5-dichlorobenzyl)piperazin-1-yl)methyl)-3-(4-(trifluoromethoxy)phenyl)-1H-indol-1-yl)propyl)piperidine-4-carboxamide
Mol Wt: 716.26
Tags: Cancer, Apoptosis, small molecule, RGNCY-0087, 3144, pan-RAS, RAS