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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Syk-Lanraplenib
Lanraplenib

Chemical Structure : Lanraplenib

CAS No.: 1800046-95-0

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Lanraplenib (GS-9876, GS9876)

货号: PC-61380Not For Human Use, Lab Use Only.

Lanraplenib (GS-9876, GS9876) is a potent, selective, orally active Syk kinase inhibitor with IC50 of 9.5 nM.

规格 价格 库存 数量
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4580 In stock
100 mg ￥7580 In stock
200 mg ￥12800 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Lanraplenib (GS-9876, GS9876) is a potent, selective, orally active Syk kinase inhibitor with IC50 of 9.5 nM.
Lanraplenib (GS-9876) displays high selectivity on a panel of 395 nonmutant kinases, with exception JAK2 to be the most potently inhibited off-target kinase with IC50 of 120 nM.
Lanraplenib (GS-9876) is a potent inhibitor (EC50 24-51 nM) of signaling downstream of the B-cell receptor and completely abrogates the expression of the cell-surface activation markers CD86 and CD69 with EC50 112-164 nM.
Lanraplenib (GS-9876) inhibits proliferation of B-cells following BCR stimulation with IC50 of 108 nM, also reduces immune-complex (IC) stimulated release of proinflammatory cytokines from human macrophages with TNFα and IL-1β inhibited more potently than IL-6.
Lanraplenib (GS-9876) suppressed disease progression and improves survival in the NZB/W F1 murine lupus model.

物理化学性质&存储条件

分子量 443.515
分子式 C23H25N9O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

6-(6-aminopyrazin-2-yl)-N-{4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl}imidazo[1,2-a]pyrazin-8-amine

参考文献

1. Peter Blomgren, et al. ACS Med Chem Lett. 2020 Feb 12;11(4):506-513.

2. Pohlmeyer CW, et al. BMC Rheumatol. 2021 Mar 30;5(1):15.

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