GDC-0810

Research use only, not for human use.

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).

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 Cancer Phase 1 Discontinued

ARN-810;Brilanestrant

Endocrinology/Hormones

Estrogen Receptor/ERR

ERα

Cancer

Breast Cancer

1365888-06-7

446.90

C26H20ClFN2O2

>98% (HPLC)

DMSO: ≥ 30 mg/mL

CCC(=C(C1=CC=C(C=C1)C=CC(=O)O)C2=CC3=C(C=C2)NN=C3)C4=C(C=C(C=C4)F)Cl

2-Propenoic acid, 3-[4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)-1-buten-1-yl]phenyl]-, (2E)-

(-20℃)

With Ice Pack

≥ 2 years