OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC 50 of 1.6 and 3.2?nM, respectively.
性状
Solid
IC50 & Target[1][2]
ERα ERβ
体外研究(In Vitro)
OP-1074 (0-100?nM; 24 hours) inhibits MCF-7 cells and CAMA-1 cells proliferation with IC50 values of 6.3 and 9.2 nM, respectively.OP-1074 (100?nM; 24 hours) destabilizatizes ERα protein expression in MCF-7 and CAMA-1 cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
参考文献
[1]. Fanning SW, et al. Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.Nat Commun. 2018 Jun 18;9(1):2368.
溶解度数据
In Vitro: DMSO : 100 mg/mL (218.55 mM; Need ultrasonic)配制储备液
[1]. Fanning SW, et al. Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.Nat Commun. 2018 Jun 18;9(1):2368.