Darovasertib

SKU: orb1301656

Description

Darovasertib (LXS196) is a potent, selective, and orally bioavailable inhibitor of protein kinase C (PKC), demonstrating high selectivity for PKCα and PKCθ over GSK3β. It is a valuable research tool for investigating PKC signaling in oncology, particularly in uveal melanoma models, both in vitro and in vivo.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1874276-76-2
• MW: 472.47
• Purity: 99.89% (May vary between batches)
• Formula: C₂₂H₂₃F₃N₈O
• SMILES: CC1(N)CCN(CC1)c1cccnc1NC(=O)c1nc(cnc1N)-c1ncccc1C(F)(F)F
• Target: PKC
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.47 mM);DMSO:16.67 mg/mL (35.28 mM)

Bioactivity

• Target IC50:
  PKCα:1.9 nM |PKCθ:0.4 nM |GSK-3β:3.1 μM
• In Vitro:
  An orally available protein kinase C (PKC) inhibitor with potential immunosuppressive and antineoplastic activities. Upon oral administration, protein kinase C inhibitor Darovasertib 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Darovasertib, inhibit, LXS 196, LXS196, LXS-196, IDE 196, IDE196, IDE-196, Inhibitor, Protein kinase C, PKC

Compound Identifiers

PubChem CID

118873253