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Lanraplenib

Catalog No. T11824LL   CAS 1800046-95-0
Synonyms: GS-9876

Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.

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Lanraplenib Chemical Structure
Lanraplenib, CAS 1800046-95-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 47.00
2 mg In stock $ 68.00
5 mg In stock $ 101.00
10 mg In stock $ 170.00
25 mg In stock $ 306.00
50 mg In stock $ 453.00
100 mg In stock $ 667.00
1 mL * 10 mM (in DMSO) In stock $ 117.00
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Purity: 99.42%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
Targets&IC50 Syk:9.5 nM
In vitro Lanraplenib (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]. Lanraplenib inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK, ERK, MEK, and PKCδ in human B cells (EC50s: 24-51 nM). Lanraplenib 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, Lanraplenib inhibits IC-stimulated TNFα and IL-1β release (EC50: 121±77 nM and 9±17 nM, respectively) [1].
Synonyms GS-9876
Molecular Weight 443.5
Formula C23H25N9O
CAS No. 1800046-95-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 41.67 mg/mL (93.96 mM), Sonication is recommended.

TargetMolReferences and Literature

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).

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Inhibitor Library Kinase Inhibitor Library Bioactive Compound Library ReFRAME Related Library Angiogenesis related Compound Library Orally Active Compound Library Bioactive Compounds Library Max

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Keywords

Lanraplenib 1800046-95-0 Angiogenesis Tyrosine Kinase/Adaptors Syk Spleen tyrosine kinase Inhibitor GS9876 GS-9876 GS 9876 inhibit inhibitor

 

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