LXG6403 hydrochloride is a highly potent, competitive and irreversible lysyl oxidase (LOX) inhibitor (IC50 value of 1.3 µM) with ∼3.5-fold specificity for LOX compared to LOXL2 while not inhibiting LOXL1. LXG6403 shows favorable pharmacokinetic properties, globally changes ECM/collagen architecture, and reduces tumor stiffness. This leads to better drug penetration, inhibits FAK signaling, and induces ROS/DNA damage, G1 arrest, and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines, PDX organoids, and in vivo.

KEYWORDS: LXG6403 hydrochloride | Supplier | LOX inhibitor | LXG 6403 | LXG-6403 | CAS [315705-04-5] | Lysine | Inhibitor | Enzymes | TNBC | Lysyl oxidase