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Compound and application thereof

A compound and tumor technology, applied in the field of biomedicine, can solve the problem of low proportion of clinical beneficiaries

Active Publication Date: 2022-04-12
LETO LAB CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Immunotherapy, such as immune checkpoint inhibitors, has been a research hotspot in recent years, and has made good breakthroughs in the fields of melanoma, kidney cancer, lung cancer, liver cancer, etc., but the low proportion of clinical benefit population is a problem that needs to be solved in the future

Method used

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  • Compound and application thereof
  • Compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1 compound preparation

[0015] Take an appropriate amount of Fmoc-Ser(tbu)-wang resin with a substitution degree of about 0.3mmol / g, place it in a solid-phase reactor, add an appropriate amount of DMF to wash once, then use DCM to swell for 10-15min, remove the DCM, and add an appropriate amount of DBLK solution for deprotection 2 times (10min+15min). Wash once with DMF in between. After deprotection, rinse with appropriate amount of DMF 6 times. Take a small amount of resin and add Kaiser reagent indene dropwise for detection. If the resin is blue, continue the experiment; if the resin is colorless, repeat the above deprotection steps. Take 3eq of Fmoc-D-Tyr(tbu)-OH and 3eq of HBTU, put them in a reactor, add an appropriate amount of DMF to dissolve, then add 3eq of DIEA dropwise to start the reaction. React at room temperature for 1 hour, rinse with an appropriate amount of DMF for 3 times, take a small amount of resin and dropwise add Kaiser's reagent ...

Embodiment 2

[0017] Embodiment 2 anti-breast cancer effect

[0018] MDA-MB-231 human breast cancer tumor cells were derived from ATCC. NCG-hIL15 mice were obtained from Jiangsu Jicui Yaokang Biotechnology Co., Ltd. MDA-MB-231 tumor cells were inoculated subcutaneously in tumor-donor mice, and after the tumor grew, a volume of about 500-1000 mm was taken out under sterile conditions 3 The tumor was cut into small pieces with a size of about 2mm×2mm×2mm, and inoculated subcutaneously on the right flank of the experimental mice with a trocar, and each mouse was inoculated with one tumor mass. PBMC were derived from normal human peripheral blood, inoculated into tumor-bearing mice, 2×10 6 / mouse. When the average tumor volume reaches 50-70mm 3 Dosing in groups (recorded as PG-D0 on the same day), 6 rats in each group, 2 groups in total, PBS group and compound Ⅰ group, intraperitoneal injection, once a day, continuous administration for 21 days, dosage 50mg / kg . After grouping until the e...

Embodiment 3

[0020] Embodiment 3 anti-colorectal cancer effect

[0021] CT26 cells were cultured in RPMI1640 medium containing 10% fetal bovine serum. Cells in exponential growth phase were collected and resuspended in PBS to a suitable concentration for subcutaneous tumor inoculation. BALB / C mice were subcutaneously inoculated with 5*10 5 Cells, the cells were resuspended in PBS (0.1ml / only), and the tumor growth was observed regularly until the tumor grew to an average volume of 60-80mm 3 The mice were randomly divided into groups according to tumor size and body weight. The day of tumor cell inoculation was defined as day 0. 6 rats in each group, 2 groups in total, PBS group and compound Ⅰ group, intraperitoneal injection, once a day, continuous administration for 21 days, the administration dose was 50 mg / kg. After grouping until the end of the experiment, the tumor volume was measured twice a week using a vernier caliper to measure the long diameter and short diameter of the tumor...

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PUM

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Abstract

The invention belongs to the technical field of biological medicines, and particularly discloses a compound and application thereof. The tumors include but are not limited to breast cancer, bladder cancer, colorectal cancer, liver cancer, lung cancer, lymphoma, myeloma, leukemia, melanoma, brain tumor, pancreatic cancer, prostate cancer, kidney cancer, ovarian cancer, head and neck cancer, nasopharynx cancer, esophagus cancer, gallbladder cancer, bile duct cancer, cervical cancer, stomach cancer, mesothelioma, glioblastoma, neuroblastoma, uterine cancer and thyroid cancer. , sarcoma, skin cancer, osteoma, osteosarcoma, testicular cancer, spermatocytoma, ureteral tumor, chorioepithelial cancer, and the like. In-vivo tumor pharmacological experiments prove that the compound disclosed by the invention has an obvious broad-spectrum anti-tumor effect.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to a compound and its application. Background technique [0002] Cancer is a major public health problem worldwide, seriously threatening human health, and its morbidity and mortality are increasing. In January 2021, the International Agency for Research on Cancer (IARC) released the 2020 Global Cancer Statistics Report, which counted and analyzed 36 cancers in 185 countries and regions around the world. In 2020, there will be approximately 19.3 million new cancer cases worldwide (approximately 18.1 million cases after excluding non-melanoma skin cancers), and nearly 10 million patients will die from cancer (approximately 9.9 million cases after excluding non-melanoma skin cancers). Compared with the data in 2018 (18.1 million new cases and 9.6 million deaths), it has increased, resulting in a huge population loss and a heavy economic and medical burden. As the popul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/065A61K38/05A61P35/00
Inventor 张维
Owner LETO LAB CO LTD
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