SKLB-850(SKLB-850) - 药物靶点：JAK2 x SRC x Syk_专利_临床

概要

基本信息

药物类型

化学药

别名

靶点

JAK2 x SRC x Syk

作用机制

JAK2抑制剂(酪氨酸蛋白激酶JAK2抑制剂)、SRC抑制剂(酪氨酸蛋白激酶SRC抑制剂)、Syk抑制剂(脾酪氨酸激酶抑制剂)

治疗领域

肿瘤免疫系统疾病血液及淋巴系统疾病

在研适应症-

非在研适应症

B细胞淋巴瘤

原研机构

四川大学华西第二医院

在研机构-

非在研机构

四川大学华西第二医院

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)无进展

特殊审评-

关联

100 项与 SKLB-850 相关的临床结果

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100 项与 SKLB-850 相关的转化医学

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100 项与 SKLB-850 相关的专利（医药）

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1

项与 SKLB-850 相关的文献（医药）

2017-12-19·Oncotarget

A novel orally available Syk/Src/Jak2 inhibitor, SKLB-850, showed potent anti-tumor activities in B cell lymphoma (BCL) models

Article

作者: Ji, Sen ; Ma, Yu ; Zhu, Jun ; Lin, Wanting ; Zheng, Mingwu ; Zhang, Nannan ; Li, Jiong ; Liang, Xiao ; Li, Lin-Li ; Wei, Yu-Quan ; Yang, Sheng-Yong ; Chen, Kai ; Liu, Ning ; Zhang, Guo ; Li, Guobo ; Niu, Ting

B cell lymphoma (BCL) is the most frequently diagnosed type of non-Hodgkin lymphoma (NHL), and accounts for about 4% of all cancers in the USA. Kinases spleen tyrosine kinase (Syk), Src, and Janus kinase 2 (JAK2) have been thought as potential targets for the treatment of BCL. We have recently developed a multikinase inhibitor, SKLB-850, which potently inhibits Syk, Src, and JAK2. The aim of this study is to investigate the anti-BCL activities and mechanisms of action of SKLB-850 both in vitro and in vivo. Our results showed that SKLB-850 significantly inhibited BCL cell proliferation, and induced apoptosis of BCL cells. It could considerably decrease the secretion of chemokines CCL3, CCL4, and CXCL12. Oral administration of SKLB-850 considerably suppressed the tumor growth in BCL xenograft models (Ramos and HBL-1) in a dose-dependent manner. Immunohistochemistry of tumor tissues showed that SKLB-850 efficiently inhibited the activation of Syk/ERK, Src/FAK and JAK2/Stat3 pathways. Collectively, SKLB-850 could be a promising agent for the treatment of BCL, hence deserving further study.

100 项与 SKLB-850 相关的药物交易

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