Sovleplenib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Sovleplenib (HMPL-523) 是一种高效的、可口服的选择性 SYK 抑制剂，IC50 为 25 nM。具有抗肿瘤活性。Sovleplenib 可用于免疫性血小板减少症（ITP）的研究。

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 中的溶解度 : 25 mg/mL (51.80 mM; 超声助溶 (<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