Lanraplenib (GS-9876)

Modify Date: 2024-01-09 15:29:39

Lanraplenib (GS-9876) structure	Common Name	Lanraplenib (GS-9876)
	CAS Number	1800046-95-0	Molecular Weight	443.50
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₃H₂₅N₉O	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Lanraplenib (GS-9876)

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	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Syk Research Areas >> Inflammation/Immunology
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	[1]. Di Paolo J, et al. FRI0049 Preclinical Characterization of GS-9876, A Novel, Oral SYK Inhibitor That Shows Efficacy in Multiple Established Rat Models of Collagen-Induced Arthritis.Annals of the Rheumatic Diseases 2016;75:443-444. [2]. Clarke AS, et al. Effects of GS-9876, a novel spleen tyrosine kinase inhibitor, on platelet function and systemic hemostasis. Thromb Res. 2018 Oct;170:109-118. [3]. Kivitz AJ, et al. GS-9876, a Novel, Highly Selective, SYK Inhibitor in Patients with Active Rheumatoid Arthritis: Safety, Tolerability and Efficacy Results of a Phase 2 Study [abstract]. Arthritis Rheumatol.2018; 70 (suppl 10).

Molecular Formula	C₂₃H₂₅N₉O
Molecular Weight	443.50

DC Chemicals Limited
China
Product Name: Lanraplenib (GS-9876)
Price: $950.0/100mg $1500.0/250mg $2700.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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