Unlock instant, AI-driven research and patent intelligence for your innovation.

Application of OSI-906

A technology of OSI-906, 1. OSI-906, applied in the application field of OSI-906, can solve the problem of thyroid eye disease and the like that there is no IGF-1R small molecule inhibitor

Inactive Publication Date: 2021-07-23
SUZHOU PRO HEAL PHARM TECH CO LTD
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the research on the application of OSI-906 is mostly aimed at the treatment of certain tumors and cancers, and there is no report on the use of IGF-1R small molecule inhibitors in the treatment of thyroid eye disease

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of OSI-906
  • Application of OSI-906
  • Application of OSI-906

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Inhibitory effect of OSI-906 on IGF-1R

[0035] The overexpression and activation of IGF-1R can promote the proliferation of tumor cells, and the IC of the compound on the inhibition of cell proliferation can be detected by adding different concentrations of the compound 50 result. OSI-906 was diluted to different final concentrations and co-cultured with human breast cancer cells MCF-7 in 96-well plates for 3 days, the serum concentration was 10%, and the growth inhibition of cells was detected by CellTiterGlo instrument. The IC of OSI-906 was obtained by calculating and fitting the corresponding relationship between different concentrations of OSI-906 and the number of cells (calculated by the measured fluorescence intensity of extracellular ATP). 50 The value is 177nM.

Embodiment 2

[0036] Example 2 The efficacy of OSI-906 in animal models of hyperthyroidism

[0037]Rat models of hyperthyroidism and thyroid-related eye disease were induced by intraperitoneal injection of bovine thyroglobulin, and the effect of OSI-906 on rat thyroid-related eye disease was observed, including the following steps:

[0038] (1) Adult healthy male SD rats were selected and randomly divided into 3 groups, ten rats in each group, which were normal control group, model-making control group and model-making administration group. Rats in the model group were injected with bovine thyroglobulin intraperitoneally at a dose of 150 μg / rat every 2 weeks to establish the model, and the model was completed for 4 weeks. The specific dosage regimen is operated according to Table 1:

[0039] Table 1

[0040]

[0041] (2) Animals were euthanized 4 weeks after administration and samples were collected. After the rats were euthanized, the extraocular muscles were collected, stained, and ...

Embodiment 3

[0045] Example 3 The efficacy of OSI-906 in animal models of polycystic ovary syndrome

[0046] The model of polycystic ovary syndrome was established by subcutaneous injection of dihydrotestosterone in SD female rats, and the evaluation of OSI-906 in the model was selected by monitoring the changes in rat weight gain, the number of atresic follicles, and the changes in epithelial cells in vaginal smears. The efficacy of the drug, specifically including the following steps:

[0047] (1) Select adult healthy female SD rats with similar days of birth and body fat, and divide them into 3 groups randomly, ten rats in each group, which are normal control group, modeling control group and modeling administration group respectively. After grouping, each There was no significant difference in the body weight of rats in the two groups. Rats in the model group were raised under the same conditions, and the rats in the model group were subcutaneously injected with dihydrotestosterone at...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides application of OSI-906, and relates to the field of biological medicine. OSI-906 is a small molecule compound, can inhibit signal transduction, proliferation and cytokine secretion of a tyrosine kinase receptor IGF-1R in a human body, and can be used for treating related diseases; for example, thyroid-related eye diseases, inflammatory skin diseases, systemic mucoedema, tibialis anterior mucoedema, polycystic ovarian syndrome, hyperandrogenemia, endometriosis-related pain, systemic sclerosis and the like.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to an application of OSI-906. Background technique [0002] IGF-1R belongs to the tyrosine protein kinase receptor family. It is a transmembrane protein on the cell surface and can be activated by IGF-1 and IGF-2 (both insulin growth factors). Its overexpression may be related to multiple sclerosis, Crohn's disease, pulmonary fibrosis and other malignant tumors and autoimmune diseases are related. Insulin growth factor 1 receptor (IGF-1R) inhibitors can act as selective inhibitors against cancer cell growth. In recent years, small molecule kinase inhibitors targeting IGF-1R have developed rapidly. [0003] OSI-906 is a novel small molecule IGF-1R inhibitor discovered by researchers in the field, which can effectively and selectively inhibit the autophosphorylation of IGF-1R by blocking the MAPK and PI3K-Akt pathways. In vivo experiments, OSI-906 has a significant inhibitory effect on the ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4985A61P27/02A61P29/00A61P17/00A61P15/00
CPCA61K31/4985A61P27/02A61P29/00A61P17/00A61P15/00
Inventor 张鹏马琳郭树华
Owner SUZHOU PRO HEAL PHARM TECH CO LTD