LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. It can be used for the treatment of uveal melanoma[1][2].
Upon oral administration, protein kinase C inhibitor LXS196 binds to and inhibits PKC, which prevents the activation of PKC-mediated signaling pathways. This may lead to the induction of cell cycle arrest and apoptosis in susceptible tumor cells. PKC, a serine/threonine protein kinase overexpressed in certain types of cancer cells, is involved in tumor cell differentiation, proliferation, invasion and survival[1].
LXS196 (compound 9) (15, 30, 75, 150 mg/kg, P.O., mice) shows improved efficacy (regression) in a 92.1 GNAQ uveal melanoma xenograft model in a dose-dependently manner[2].|| Animal Model:|Mice implanted with 92.1 GNAQ mutant uveal melanoma cells[2].|Dosage:|15, 30, 75, 150 mg/kg|Administration:|P.O. (bid) for 35 days|Result:|Dose-dependently suppressed the tumor growth.
[1]. Protein Kinase C Inhibitor LXS196 [2]. US20180179181.