A kind of non-ATP competitive FGFR1 inhibitor and its application

A technology of FGFR1 and inhibitor, applied in the field of pharmacy, can solve the problems of large toxic and side effects, poor targeting selectivity, etc.
CN106995368BActive Publication Date: 2020-12-04WENZHOU MEDICAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
WENZHOU MEDICAL UNIV
Publication Date
2020-12-04

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Abstract

The invention belongs to the field of pharmacy and particularly relates to application of a specific non-ATP-competiveness FGFR1 (fibroblast growth factor receptor 1) inhibitor in preparing anticancer medicine and medicine for treating cancer-related diseases. The invention further relates to a small molecule compound L16H50 which can inhibit FGFR1 and activation of a signal channel of the FGFR1 in a non-ATP-dependent mode. Therefore, multiplication and survival of cancer cells are inhibited, and good in-vitro and in-vivo anticancer effects are further given to play.
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Description

technical field

[0001] The present invention belongs to the field of pharmacy. Specifically, the present invention relates to a small molecular compound that can inhibit the activation of FGFR1 and its signaling pathway in an ATP-independent manner, thereby exerting good anti-tumor effects in vivo and in vitro. Background technique

[0002] FGFR1, namely fibroblast growth factor receptor 1, is a member of the fibroblast growth factor (FGF) family and belongs to the tyrosine receptor kinase. A large number of studies have proved that FGFR1 is closely related to a variety of tumors, such as gastric cancer. In gastric cancer, the expression of FGFR1 is related to the 10-year survival rate and distant metastasis of tumors. Such as lung cancer, studies have shown that the expression of FGFR1 can be used as a prognostic marker for non-small cell lung cancer. In breast cancer, amplification of the region of chromosome 8p11-12 (and the region where FGFR1 is located) occurs in 10% o...

Claims

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