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Brilanestrant

Catalog No. T5118 CAS 1365888-06-7

Synonyms: GDC0810, GDC 0810, GDC-0810, ARN-810, RG 6046

Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM).

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Brilanestrant, CAS 1365888-06-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
2 mg	In stock	$ 70.00
5 mg	In stock	$ 108.00
10 mg	In stock	$ 153.00
25 mg	In stock	$ 273.00
50 mg	In stock	$ 450.00
100 mg	In stock	$ 647.00
1 mL * 10 mM (in DMSO)	In stock	$ 129.00

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Purity: 98.71%

Purity: 98.54%

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Description	Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM).
Targets&IC50	ERα:0.7 nM
In vitro	GDC-0810 is a ERα 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]. 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].
In vivo	The pharmacokinetic profile of GDC-0810 shows it is a clearance molecule across species, with good bioavailability (40%-60%). GDC-0810 (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]. GDC-0810 exhibits low clearance (11 mL/min/kg) and 61% oral bioavailability. GDC-0810 (1-100 mg/kg/day, p.o.) displays dose-dependent efficacy in the MCF7 xenograft model [2].
Cell Research	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.
Animal Research	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.

Synonyms	GDC0810, GDC 0810, GDC-0810, ARN-810, RG 6046
Molecular Weight	446.9
Formula	C26H20ClFN2O2
CAS No.	1365888-06-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (123.07 mM)

H2O: Insoluble

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Bioactive Compound Library Clinical Compound Library Bioactive Compounds Library Max Anti-Ovarian Cancer Compound Library Orally Active Compound Library NO PAINS Compound Library

Related Products

Related compounds with same targets

Pipendoxifene hydrochloride Quinestrol Bazedoxifene hydrochloride β-Estradiol 17-acetate Dihydroresveratrol Endoxifen (E-isomer) Estrogen receptor modulator 10 G36

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Keywords

Brilanestrant 1365888-06-7 Endocrinology/Hormones Estrogen/progestogen Receptor Estrogen Receptor/ERR GDC0810 inhibit ARN810 GDC 0810 RG6046 Inhibitor GDC-0810 RG-6046 ARN 810 ARN-810 RG 6046 inhibitor

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