Sovleplenib

Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC₅₀ of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP)^[1]. IC50 & Target: SYK^[1] In Vitro: Sovleplenib (HMPL-523) inhibits SYK, FLT3, KDR, LYN, FGFR2, and AUR A with IC₅₀s of 0.025, 0.063, 0.390, 0.921, 3.214, 3.969 μM, respectively^[1].
Sovleplenib (HMPL-523) blocks phosphorylation of BLNK, downstream protein of Syk, in human mantle cell line REC-1 and human plasma cell line ARH-7777 with IC₅₀s of 0.105 µM and 0.173 μM, respectively^[2].
Sovleplenib also inhibits cell viability of Ba/F3 Tel-Syk with the IC₅₀ of 0.033 μM^[2].
Sovleplenib also increases the apoptotic rate of REC-1 cells^[2].
Sovleplenib shows the synergistic activities on killing human diffused large B cell lymphoma (DLBCL) in combination with other drugs such as BTK inhibitor, PI3Kδ inhibitors and Bcl2 family inhibitor^[2]. In Vivo: Sovleplenib (HMPL-523) shows anti-tumor activity in vivo. Sovleplenib (100 mg/kg) inhibits tumor growth in REC-1 subcutaneous xenograft model^[1].
Sovleplenib (HMPL-523; 100 mg/kg; daily oral administration) shows potent anti-tumor activity in B cell lymphoma REC-1 (TGI: 59%) in Syk dependent xenograft models ^[2].