Entospletinib (GS-9973) - 98%, high purity , Tyrosine-protein kinase SYK inhibitor, CAS No.1229208-44-9, Tyrosine-protein kinase SYK inhibitor

Item Number

E413770

• Synonyms: Entospletinib | 1229208-44-9 | GS-9973 | 6-(1H-Indazol-6-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazin-8-amine | Entospletinib [INN] | Entospletinib (GS-9973) | gs9973 | GS9973Entospletinib | 6I3O3W6O3B | CHEMBL3265032 | SYK INHIBITOR GS-9973 | 6-(1H-Indazol-6-yl)-N-(4-(morp
• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay and showed 13- to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Tyrosine-protein kinase SYK inhibitor

Product Description

Information

Entospletinib (GS-9973) Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay and showed 13- to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.

Targets

Syk (Cell-free assay) 7.7 nM

In vitro

GS-9973 shows good bidirectional permeability across Caco-2 cell monolayers in vitro. In cells, GS-9973 also shows excellent selectivity for Syk, and potently inhibits BCR-mediated activation and proliferation of B-cells as well as immune-complex-stimulated cytokine production in monocytes. The combination of idelalisib and GS-9973 synergistically inhibits CLL cell viability and further disrupts chemokine signaling.

In vivo

GS-9973 (1 mg/kg p.o.) shows moderate to high bioavailability in rat and dog. In a rat collagen-induced arthritis model, GS-9973 (1-10 mg/kg p.o.) significantly inhibits ankle inflammation. Moreover, GS-9973 also shows disease-modifying activity in multiple histological measurements, including inhibition of pannus formation, cartilage damage, bone resorption, and peritosteal bone formation with ED50 ranging from 1.2 to 3.9 mg/kg .

Cell Research(from reference)

Cell lines：MV-4-11 cells 

Concentrations：~10 μM 

Incubation Time：72 hours