ARN-810; GDC-0810 MedChemExpress (MCE)

Product Name	GDC-0810
Synonyms	CS-2080 ARN-810 GDC-0810 BRILANESTRANT GDC-0810(ARN-810) GDC-0810 (Brilanestrant) (E)-3-(4-((E)-2-(2-CHLORO-4-FLUOROPHENYL)-1-(1H-INDAZOL-5-YL)BUT-1-EN-1-YL)PHENYL)ACRYLIC ACID Synonyms CS-2080 ARN-810 GDC-0810 BRILANESTRANT GDC-0810(ARN-810) GDC-0810 (Brilanestrant) (E)-3-(4-((E)-2-(2-CHLORO-4-FLUOROPHENYL)-1-(1H-INDAZOL-5-YL)BUT-1-EN-1-YL)PHENYL)ACRYLIC ACID (E)-3-[4-[(E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl]phenyl]-2-propenoic acid
CAS	1365888-06-7
EINECS
Chemical Formula	C26H20ClFN2O2
Molecular Weight	446.9
inchi
Package	10 mM * 1 mL;2 mg;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	Brilanestrant Brilanestrant MedChemExpress (MCE) HY-12864 1365888-06-7 ARN-810 Descriptions Brilanestrant Brilanestrant MedChemExpress (MCE) HY-12864 1365888-06-7 ARN-810 GDC-0810 99.95% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Brilanestrant (ARN-810 GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM. Brilanestrant (ARN-810 GDC-0810) 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 GDC-0810) 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]. Time release pellets containing 0.72 mg 17-β estradiol are subcutaneously implanted into nu/nu mice. MCF-7 cells are grown in RPMI containing 10% FBS at 5% CO2 37°C. Trypsinized cells are pelleted and resuspended in 50% RPMI（serum free）and 50% Matrigel at 1×107 cells/mL. MCF-7 cells are subcutaneously injected (100 μL/animal) on the right flank 2-3 days post pellet implantation. Tumor volume (length × width2/2) is monitored biweekly. When tumors reach an average volume of appr 200 mm3 animals are randomized and treatment is started. Animals are treated with vehicle or compound daily for 4 weeks. Tumor volume and body weight are monitored biweekly throughout the study. MCF-7 cells are adjusted to a concentration of 40000 cells per mL in RPMI containing 10% FBS and 20 mM HEPES. Then 16 μL of the cell suspension (640 cells) is added to each well of a 384-well plate, and the cells are incubated overnight to allow the cells to adhere. The following day a 10-point, serial 1:5 dilution of each compound is added to the cells in 16 μL at a final concentration ranging from 10 to 0.000005 μM. After 5 days' compound exposure, 16 μL of CellTiter-GLo is added to the cells, and the relative luminescence units of each well are determined. CellTiter-GLo added to 32 μL of medium without cells is used to obtain a background value. The percent viability of each sample is determined as follows: (RLU sample-RLU background/RLU untreated cells-RLU background ×100=%viability) IC50: 0.7 nM (estrogen receptor) Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [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 [Content Brief]
Last Update	2025-04-01 14:45:47

MedChemExpress (MCE) also provides

Thalidomide-4-O-C2-NH2

Category: Signaling Pathways
CAS: 2341840-99-9
Last Update: 2025-04-01 14:45:47

PPARα-MO-1

Category: Signaling Pathways
CAS: 810677-36-2
Last Update: 2025-04-01 14:45:47

Netupitant N-oxide

Category: Signaling Pathways
CAS: 910808-11-6
Last Update: 2025-04-01 14:45:47

MK-0812

Category: Signaling Pathways
CAS: 624733-88-6
Last Update: 2025-04-01 14:45:47

TS-011

Category: Signaling Pathways
CAS: 339071-18-0
Last Update: 2025-04-01 14:45:47

SCH 530348 sulfate

Category: Signaling Pathways
CAS: 705260-08-8
Last Update: 2025-04-01 14:45:47

BAG 956

Category: Signaling Pathways
CAS: 853910-02-8
Last Update: 2025-04-01 14:45:47

YM758

Category: Signaling Pathways
CAS: 312752-85-5
Last Update: 2025-04-01 14:45:47


Supplier Name	MedChemExpress (MCE)
Contact	sales
Tel	609-228-6898
Mobile	609-228-6898
QQ
Email	sales@medchemexpress.com; tech@medchemexpress.com
Website	https://www.medchemexpress.com/
Wechat

Request for quotation

Supplier Contact