
Entospletinib
CAS No. 1229208-44-9
Entospletinib( Entospletinib | GS9973 | GS 9973 )
Catalog No. M17895 CAS No. 1229208-44-9
Entospletinib (IC50= 7.7 nM)is a specific Syk inhibitor, which is orally bioavailable.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 41 | In Stock |
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5MG | 67 | In Stock |
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10MG | 88 | In Stock |
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25MG | 160 | In Stock |
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50MG | 245 | In Stock |
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100MG | 394 | In Stock |
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200MG | 584 | In Stock |
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500MG | Get Quote | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameEntospletinib
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NoteResearch use only, not for human use.
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Brief DescriptionEntospletinib (IC50= 7.7 nM)is a specific Syk inhibitor, which is orally bioavailable.
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DescriptionEntospletinib, also known as GS-9973, is a highly selective and orally efficacious Syk inhibitor which is currently undergoing clinical evaluation for autoimmune and oncology indications. In Phase II clinical trials, Entospletinib demonstrates clinical activity in subjects with relapsed or refractory CLL with acceptable toxicity.(In Vitro):Entospletinib (GS-9973) shows good bidirectional permeability across Caco-2 cell monolayers in vitro. In cells, Entospletinib (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 Entospletinib (GS-9973) synergistically inhibits CLL cell viability and further disrupts chemokine signaling.(In Vivo):Entospletinib (GS-9973) (1 mg/kg, p.o.) shows moderate to high bioavailability in rat and dog. In a rat collagen-induced arthritis model, Entospletinib (GS-9973) (1-10 mg/kg, p.o.) significantly inhibits ankle inflammation. Moreover, Entospletinib (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.
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In Vitro——
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In Vivo——
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SynonymsEntospletinib | GS9973 | GS 9973
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PathwayGPCR/G Protein
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TargetAntibacterial
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RecptorSyk
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1229208-44-9
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Formula Weight411.47
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Molecular FormulaC23H21N7O
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 43 mg/mL; 104.51 mM
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SMILESC1CN(CCO1)c1ccc(Nc2nc(cn3ccnc23)c2ccc3cn[nH]c3c2)cc1
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Chemical Name6-(1H-indazol-6-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazin-8-amine
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Currie KS, et al. Discovery of GS-9973, a Selective and Orally Efficacious Inhibitor of Spleen Tyrosine Kinase. J Med Chem. 2014 May 8;57(9):3856-73.
molnova catalog



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