Sovleplenib(Synonyms: HMPL-523)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Sovleplenib (Synonyms: HMPL-523)

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(Synonyms: HMPL-523)

Sovleplenib Chemical Structure

CAS No. : 1415792-84-5

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生物活性

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]
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c nude mice bearing subcutaneously implanted REC-1 cells or intravenously injected BA/F3 cells or BA/F3 TEL-SYK cells[1]
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.

分子量

482.60

Formula

C24H30N6O3S
CAS 号

1415792-84-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Su WG, et al. Preparation of pyridopyrazine derivatives for use as Syk inhibitors. WO2012167733 A1.

    [2]. Na Yang, et al. HMPL-523, a Novel SYK Inhibitor Showed Anti-Tumor Activities In Vitro and In Vivo. Blood (2016) 128 (22): 3970.

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