2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
GDC-0810 (ARN-810, Brilanestrant) is a non-steroidal, orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM (ER-α degradation), binds to ERα and ERβ with with Ki of 3.8 and 3.7 nM, respectively; dually antagonizes and induces proteasome-dependent degradation of ERα, exhibits robust in vitro activity against a variety of human breast cancer cell lines (MCF7 cell IC50=25 nM); demonstrates robust activity in models of tamoxifen-sensitive and tamoxifen-resistant breast cancer models.Breast CancerPhase 1 Discontinued
