Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor 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.
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| Name | Lanraplenib |
|---|---|
| Iupac Chemical Name | 6-(6-aMinopyrazin-2-yl)-n-{4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl}imidazo[1,2-a]pyrazin-8-amine |
| Synonyms | Lanraplenib ; GS-SYK ; GS-9876 ; GS 9876 ; GS9876; |
| Molecular Formula | C23H25N9O |
| Molecular Weight | 443.50 |
| Smile | NC1=CN=CC(=N1)C=1N=C(C=2N(C1)C=CN2)NC2=CC=C(C=C2)N2CCN(CC2)C2COC2 |
| InChiKey | XCIGZBVOUQVIPI-UHFFFAOYSA-N |
| InChi | InChI=1S/C23H25N9O/c24-21-12-25-11-19(28-21)20-13-32-6-5-26-23(32)22(29-20)27-16-1-3-17(4-2-16)30-7-9-31(10-8-30)18-14-33-15-18/h1-6,11-13,18H,7-10,14-15H2,(H2,24,28)(H,27,29) |
| CAS Number | 1800046-95-0 |
| Related CAS |
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping. |
| HS Code |
| Targets | SYK Inhibitor |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study | Phase 2 |
[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).