产品描述
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[1][2].
体外活性
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[1].
体内活性
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[1].
Cas No.
2222354-91-6
分子式
C59H73N5O10S
分子量
1044.3
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years