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编 号:F279316
分子式:C59H73N5O10S
分子量:1044.3
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生物活性:
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.

体内研究:
SNIPER(ER)-87 (30 mg/kg, i.p., every 24 h for 14 days) inhibits the growth of MCF-7 orthotopic breast tumor xenografts in 6-week-old female BALB/c nude mice.

体外研究:
SNIPER(ER)-87 (0.1-1000 nM; 72 hours) efficiently inhibits the ERα-dependent transcriptional activation by β-estradiol and suppresses the growth of ERα-positive breast tumor cells with IC50s of 15.6 nM in MCF-7 and 9.6 nM in T47D cells.
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