Lanraplenib

SKU: orb1309494

Description

Lanraplenib (GS-9876) is a potent and selective oral inhibitor of spleen tyrosine kinase (SYK) with an IC50 of 9.5 nM. It is being developed for inflammatory diseases and has been shown to inhibit SYK in platelet GPVI signaling without affecting bleeding time in preclinical and clinical studies.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1800046-95-0
• MW: 443.5
• Purity: 99.42% (May vary between batches)
• Formula: C₂₃H₂₅N₉O
• SMILES: Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1
• Target: Syk
• Solubility: DMSO:41.67 mg/mL (93.96 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.51 mM)

Bioactivity

• Target IC50:
  Syk:9.5 nM
• In Vitro:
  Lanraplenib (GS-9876) inhibits glycoprotein VI (GPVI)-induced phosphorylation of linker for activation of T cells and phospholipase Cγ2, platelet activation and aggregation in human whole blood, and platelet binding to collagen under arterial flow . Lanraplenib inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK, ERK, MEK, and PKCδ in human B cells (EC50s: 24-51 nM). Lanraplenib inhibits anti-IgM mediated CD69 and CD86 expression on B-cells (EC50: 112±10 nM and 164±15 nM, respectively) and anti-IgM /anti-CD40 co-stimulated B cell proliferation (EC50: 108±55 nM). In human macrophages, Lanraplenib inhibits IC-stimulated TNFα and IL-1β release (EC50: 121±77 nM and 9±17 nM, respectively) .
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Storage & Handling

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

Alternative Names

Syk, SYK, Spleen tyrosine kinase, inhibit, Lanraplenib, Inhibitor, GS9876, GS-9876, GS 9876

Compound Identifiers

PubChem CID

118161062