Lanraplenib |CAS:1800046-95-0 Probechem Biochemicals

Chemical Structure : Lanraplenib

CAS No.: 1800046-95-0

Lanraplenib (GS-9876, GS9876)

Catalog No.: 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.

Packing	Price	Stock
10 mg	$148	In stock
25 mg	$258	In stock
50 mg	$458	In stock
100 mg	$758	In stock
200 mg	$1280	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	443.515
Formula	C23H25N9O
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
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

References

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.

Lanraplenib (GS-9876, GS9876)

Biological Activity

Physicochemical Properties

References

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