Darovasertib 是一种有效的、选择性的和具有口服活性的蛋白激酶C (PKC) 抑制剂，有用于葡萄膜黑素瘤的研究潜力，对 PKCα、PKCθ 和 GSK3β 的 IC50值分别为 1.9、0.4 和 3.1 μM。

LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor(IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively).

An orally available protein kinase C (PKC) inhibitor with potential immunosuppressive and antineoplastic activities. 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.

1874276-76-2

C22H23F3N8O

472.476

LXS196

DMSO:100 mg/mL (211.65 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years