1800046-95-0
1800046-95-0 structure
- Name: Lanraplenib (GS-9876)
- Chemical Name: Lanraplenib
- CAS Number: 1800046-95-0
- Molecular Formula: C23H25N9O
- Molecular Weight: 443.50
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Syk
- Create Date: 2019-09-07 18:11:18
- Modify Date: 2024-01-09 15:29:39
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Lanraplenib (GS-9876) is a highly selective and oral SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans[1][2][3].
| Name | Lanraplenib |
|---|
| Description | Lanraplenib (GS-9876) is a highly selective and oral SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans[1][2][3]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 9.5 nM (SYK)[1] |
| In Vitro | GS-9876 inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK, ERK, MEK, and PKCδ in human B cells with EC50 values of 24-51 nM. GS-9876 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, GS-9876 inhibits IC-stimulated TNFα and IL-1β release (EC50=121±77 nM and 9±17 nM, respectively)[1]. 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[2]. |
| References |
| Molecular Formula | C23H25N9O |
|---|---|
| Molecular Weight | 443.50 |