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SIGMA-2 RECEPTOR LIGAND DRUG CONJUGATES AS ANTITUMOR COMPOUNDS, METHODS OF SYNTHESIS AND USES THEREOF
专利权人:
Washington University
发明人:
William HAWKINS,Robert MACH,Dirk SPITZER,Suwanna VANGVERAVONG,Brian VAN TINE
申请号:
US16426791
公开号:
US20200123149A1
申请日:
2019.05.30
申请国别(地区):
US
年份:
2020
代理人:
摘要:
Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described. At least one described molecular species exhibits an IC50 value below 5 □M against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo, and led to 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
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