Sovleplenib

Research use only, not for human use.

Sovleplenib (HMPL523) is an orally available, selective and potent inhibitor of the splenic tyrosine kinase SYK with an IC50 of 25 nM.Sovleplenib has antitumor activity and may be used in studies of immune thrombocytopenia (ITP).

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).

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.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. Sovleplenib also inhibits cell viability of Ba/F3 Tel-Syk with the IC50 of 0.033 μM.Sovleplenib also increases the apoptotic rate of REC-1 cells. 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.

Sovleplenib (HMPL-523) shows anti-tumor activity in vivo. Sovleplenib (100 mg/kg) inhibits tumor growth in REC-1 subcutaneous xenograft model.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 .Animal Model:Balb/c nude mice bearing subcutaneously implanted REC-1 cells or intravenously injected BA/F3 cells or BA/F3 TEL-SYK cells Dosage:10 and 100 mg/kg Administration:q.d.; for 8 days Result:Inhibited tumor growth in REC-1 subcutaneous xenograft model at 100 mg/kg.

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Angiogenesis

Syk

Syk

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1415792-84-5

482.6

C24H30N6O3S

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (51.80 mM; Ultrasonic (<60°C)

CS(=O)(=O)N1CCC(CC1)c1ccc(cc1)-c1cc2nccnc2c(NC[C@@H]2CNCCO2)n1

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(-20℃)

With Ice Pack

≥ 2 years