Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor ( IC 50 =9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans In Vitro Lanraplenib succinate (GS-9876 succinate) inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK, ERK, MEK, and PKCδ in human B cells with EC 50 values of 24-51 nM. Lanraplenib monosuccinate inhibits anti-IgM mediated CD69 and CD86 expression on B-cells (EC 50 =112±10 nM and 164±15 nM, respectively) and anti-IgM /anti-CD40 co-stimulated B cell proliferation (EC 50 =108±55 nM). In human macrophages, Lanraplenib succinate inhibits IC-stimulated TNFα and IL-1β release (EC 50 =121±77 nM and 9±17 nM, respectively). Lanraplenib succinate (GS-9876 succinate) 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 9.5 nM (SYK)
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Lanraplenib succinate
CAS number：1800047-00-0 molecular formula：C23H25N9O.3/2C4H6O4
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| Chinese alias | 琥珀酸兰拉普尼 | ||
| English alias | 6-(6-Aminopyrazin-2-yl)-N-{4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl}imidazo[1,2-a]pyrazin-8-amine succinate (2:3) | AKOS040733580 | 1800047-00-0 | QJ2PS903VZ | Lanraplenib succinate | UNII-QJ2PS903VZ | AXC04700 | LANRAPLENIB SESQUISUCCINATE | Lanraplenib s | ||
| CAS number | 1800047-00-0 | molecular formula | C23H25N9O.3/2C4H6O4 |
| molecular weight | 620.64 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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