EC330 is a leukemia inhibitory factor (LIF) inhibitor.
EC330 shows marked specificity in MCF-7 cells overexpressing LIF verses MCF-7 cells. EC330 further shows cytoskeletal disruption and targeting cancer-associated fibroblasts (CAFs) through inhibition of alpha-SMA but not beta-tubulin[1].
EC330 treatment (0.1, 0.5 and 2.5 mg/kg) dose dependently reduces tumor burden in ovarian (IGROV-1) and triple negative breast cancer (MDA-MB-231) cell xenografted mouse models as well as MDA-MB-231 PDX models. EC330 exhibits no reactivity towards thiol-cysteine residues, no off target binding to major receptors, kinases or ion channels. EC330 is orally bioavailable and found to be safe and tolerable in toxicity studies[1].
[1]. Nair HB, et al. Discovery and preclinical pharmacology of EC330: A first-in-class leukemia inhibitory factor (LIF) inhibitor