URML-3881

URML-3881 is a novel, orally administered small molecule inhibitor with **specific activity against MEK1/2 (Mitogen-activated protein kinase kinase 1 and 2)**, possessing an IC50 of 30 nM in cell-free kinase assays[1][4][10]. It was developed to overcome the solubility and pharmacokinetic limitations of earlier MEK inhibitors, with enhanced drug-like properties including optimized molecular mass, logP, and aqueous solubility due to a unique tertiary nitrogen structure[1]. URML-3881 effectively reduces ERK phosphorylation, induces apoptosis, and inhibits proliferation in vitro in clear cell ovarian cancer (CCOC) models. While single-agent URML-3881 showed strong MEK inhibition activity in preclinical testing, it had limited efficacy in vivo unless combined with cisplatin, where it significantly inhibited MAPK-mediated chemoresistance and enhanced tumor regression. Its mechanism makes it a potential adjunctive sensitizer to platinum chemotherapy, especially in cancers with MAPK pathway reliance such as CCOC[1][10]. **Developer:** University of Rochester **Primary indication:** Investigated for clear cell ovarian cancer and platinum-resistant ovarian cancer, especially as a combination therapy with platinum chemotherapies.

Other names

URML3881URML-3881URML 3881