Brilanestrant (ARN-810) (Synonyms: GDC-0810, RG-6046) |
Catalog No.GC32782 |
Brilanestrant (ARN-810) (ARN-810; GDC-0810) es un degradador selectivo del receptor de estrÓgeno (SERD) biodisponible por vÍa oral con IC50 de 0,7 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1365888-06-7
Sample solution is provided at 25 µL, 10mM.
Brilanestrant (ARN-810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
Brilanestrant (ARN-810) is a potent ER-α binder (IC50=6.1 nM), a full transcriptional antagonist with no agonism (3× ERE, IC50=2 nM), and displays good potency and efficacy in ER-α degradation (EC50=0.7 nM) and MCF-7 breast cancer cell viability (IC50=2.5 nM) assays[1]. Brilanestrant (ARN-810) induces a distinct ERα conformation versus tamoxifen and other ER therapeutics, and does not exhibit tamoxifen-like ER agonism in MCF7 cells[2].
The pharmacokinetic profile of Brilanestrant (ARN-810) shows it is a olw clearance molecule across species, with good bioavailability (40%-60%). Brilanestrant (ARN-810) (3 mg/kg, p.o.) shows substantial tumor-growth inhibition in a tamoxifen-sensitive MCF-7 xenograft model, while at the highest dose of 100 mg/kg/day, all animals show tumor regression of more than 50% without weight loss[1]. Brilanestrant (ARN-810) exhibits low clearance (11 mL/min/kg) and 61% oral bioavailability. Brilanestrant (ARN-810) (1-100 mg/kg/day, p.o.) displays dose dependent efficacy in the MCF7 xenograft model[2].
[1]. By Lai, et al. Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. J Med Chem. 2015 Jun 25;58(12):4888-904. [2]. Joseph JD, et al. The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer. Elife. 2016 Jul 13;5. pii: e15828. doi: 10.7554/eLife.15828
Average Rating: 5
(Based on Reviews and 13 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *