SRX-3207 (SRX3207) is a novel, potent, orally bioactive and dual inhibitor of Syk-PI3K with anti-tumor activity. As a first-in-class’ dual Syk/PI3K inhibitor, SRX3207 was designed for the combinatorial inhibition of Syk and PI3K in one small molecule. This chemotype demonstrates efficacy in multiple tumor models and represents a novel combinatorial approach to activate antitumor immunity.

Tamatinib (formerly known as R406) is a novel potent and ATP competitive Syk inhibitor with potential to treat immune disorders and inflammatory conditions. It inhibits Syk with an IC50 of 41 nM in cell-free assays, and strongly inhibits Syk but not Lyn, shows 5-fold less potency against Flt3. Tamatinib exhibited high efficacy in a number […]

PRT-060318 (also known as PRT318) is a novel, potent, selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment. PRT-060318 was identified as a potent inhibitor of purified Syk kinase. Syk kinase was inhibited by 92%, while the activities all other kinases retained more than 70% when PRT-060318 were evaluated at a […]

Piceatannol (also known as Astringenin; NSC-622471; trans-Piceatannol), a naturally occuring stilbene, is a potent and selective Syk inhibitor and shows ~10-fold selectivity for Srk over Lyn. It has anti-inflammatory, immunomodulatory and antiproliferative activities. Piceatannol demonstrated high in vivo anti-inflammatory activity in female BALB/c mice with dextran sulfate sodium (DSS)-induced colitis. It inhibits p56lck and syk […]

Fostamatinib (formerly also known as R788; trade name: Tavalisse), a prodrug of the active metabolite R406, is an orally bioactive, potent and selective Syk inhibitor with potential anti-inflammatory activity. It inhibits Syk with an IC50 of 41 nM in a cell-free assay. On April 17th 2018, Fostamatinib was approved by the US FDA for the […]

Entospletinib (formerly known as GS-9973) is a novel, potent, orally bioavailable, and highly selective Syk inhibitor with potential anti-inflammatory and immunomodulatory activities. It inhibits Syk with an IC50 of 7.7 nM in a cell-free assay. Entospletinib displayed high in vivo anti-inflammatory activity in Rat Collagen-Induced Arthritis (CIA) Model. In monocytes, GS-9973 inhibited immune-complex-stimulated cytokine production […]

Fostamatinib disodium (also known as R-788; R-935788; brand name: Tavalisse) is the prodrug form of the active metabolite R406. It is an orally bioactive and selective Syk inhibitor with anti-inflammatory activity. It inhibits Syk kinase with IC50 of 41 nM in a cell-free assay. As of 2018, Fostamatinib gained FDA approval to treat thrombocytopenia in […]

PRT062607 (also known as P505-15, BIIB-057) HCl is a novel, potent, highly selective and orally bioavailable small molecule Syk inhibitor with potential anti-inflammatory activity. It inhibits Syk with an IC50 of 1 nM in cell-free assays, and shows >80-fold selectivity for Syk over other kinases such as Fgr, Lyn, FAK, Pyk2 and Zap70. PRT062607 produced […]