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Lanraplenib (monosuccinate)

CAT: 0804-HY-109091ASize: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-109091ASize:1 Each
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Description
Lanraplenib monosuccinate (GS-9876 monosuccinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans[1][2][3].
CAS Number
1800046-97-2
Product Name Alternative
GS-9876 (monosuccinate)
UNSPSC
12352005
Target
Syk
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology; Cancer
Assay Protocol
https://www.medchemexpress.com/lanraplenib-monosuccinate.html
Solubility
DMSO : 125 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
C27H31N9O5
Molecular Weight
561.59
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) .
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 2