| Description | Darovasertib (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). |
| In vitro | 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. |
| Target activity | PKCα:1.9 nM , PKCθ:0.4 nM , GSK-3β:3.1 μM |
| Synonyms | LXS196 |
| molecular weight | 472.47 |
| Molecular formula | C22H23F3N8O |
| CAS | 1874276-76-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (211.65 mM) |
| References | 1. Shoushtari A N , Shoushtari A N , Khan S , et al. A Phase Ib Study of Sotrastaurin, a PKC Inhibitor, and Alpelisib, a PI3Kα Inhibitor, in Patients with Metastatic Uveal Melanoma[J]. Cancers, 2021, 13(21):5504-. |