Lanraplenib (succinate)

Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=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[1][2][3].

Product Specifications

CAS Number

[1800047-00-0]

Product Name Alternative

GS-9876 (succinate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Syk

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

https://www.medchemexpress.com/lanraplenib-succinate.html

Purity

98.09

Solubility

DMSO : 83.33 mg/mL (ultrasonic)

Smiles

NC1=CN=CC(C2=CN3C(C(NC4=CC=C(N5CCN(C6COC6)CC5)C=C4)=N2)=NC=C3)=N1.O=C(O)CCC(O)=O

Molecular Formula

C23H25N9O.3/2C4H6O4

Molecular Weight

620.64

Precautions

H302, H315, H319, H335

References & Citations

[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) .