PRT062607 Hydrochloride (P505-15 Hydrochloride) is an orally available Syk inhibitor with an IC50 of 1 nM. It inhibits inflammation and induces apoptosis, demonstrating potent antitumor activity in tumor xenograft mouse models. In vitro, it also exhibits significant activity against a variety of kinases, including Fgr, MLK1, Yes, Flt3, PAK5, Lyn, cSRC, Lck, Pyk, and FAK.
- Inhibits phosphorylation of ERK(Y204), AKT(S473), and SYK(Y352) in Ramos cells
- Inhibits BLNK Tyr84 phosphorylation
- Induces apoptosis in human whole blood
- Shows dose-dependent anti-inflammatory activity in rodent models of rheumatoid arthritis
- Inhibits B-cell activation
- Prevents tumor formation in mouse xenograft models