Art. -Nr.: HY-12864

Brilanestrant

Name: Brilanestrant
Brand: MedChemExpress
SKU: HY-12864
Price: 105.00 USD
Availability: InStock
Rating: 5 (7 reviews)

(Synonyms: ARN-810; GDC-0810)

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC₅₀ of 0.7 nM.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.85%
CAS. Nr.: 1365888-06-7
Formel: C₂₆H₂₀ClFN₂O₂
Molecular Weight:446.90

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Brilanestrant Chemical Structure

CAS. Nr.: 1365888-06-7

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC₅₀ of 0.7 nM.

IC₅₀ & Target^[1]

ERα

0.7 nM (IC₅₀)

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	0.002 μM Compound: 11l, GDC-0810, ARN-810	Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay	[PMID: 25879485]
MCF7	IC₅₀	2 nM Compound: 11l, GDC-0810, ARN-810	Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay	[PMID: 25879485]
MCF7	EC₅₀	0.0007 μM Compound: 11l, GDC-0810, ARN-810	Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay	[PMID: 25879485]
MCF7	EC₅₀	0.7 nM Compound: 11l, GDC-0810, ARN-810	Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay	[PMID: 25879485]
MCF7	EC₅₀	0.7 nM Compound: 2; ARN-810	Decrease in estrogen receptor alpha level in human MCF7 cells after 4 hrs by in-cell western assay Decrease in estrogen receptor alpha level in human MCF7 cells after 4 hrs by in-cell western assay	[PMID: 26463130]
MCF7	IC₅₀	2.5 nM Compound: 2; ARN-810	Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 5 days by celltiterGlo assay Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 5 days by celltiterGlo assay	[PMID: 26463130]
MCF7	EC₅₀	0.7 nM Compound: ARN-810; 3	Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay	[PMID: 30587451]
MCF7	IC₅₀	2.5 nM Compound: ARN-810; 3	Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation measured after 5 days by Cell-titer-Glo assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation measured after 5 days by Cell-titer-Glo assay	[PMID: 30587451]
MCF7	IC₅₀	0.85 nM Compound: 2; GDC-0810	Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis	[PMID: 32551022]
MCF7	IC₅₀	44 nM Compound: 2; GDC-0810	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by Celltiter-Glo assay	[PMID: 32551022]
MCF7	EC₅₀	17 nM Compound: 10; GDC-0810	Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay	[PMID: 34251202]
T47D	IC₅₀	1.7 nM Compound: 2; GDC-0810	Induction of ERalpha degradation in human T47D cells Induction of ERalpha degradation in human T47D cells	[PMID: 32551022]
T47D	IC₅₀	27 nM Compound: 2; GDC-0810	Antiproliferative activity against human T47D cells assessed as reduction in cell viability Antiproliferative activity against human T47D cells assessed as reduction in cell viability	[PMID: 32551022]

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1365888-06-7
Appearance Solid
Molecular Weight 446.90
Formel C₂₆H₂₀ClFN₂O₂
Color White to off-white
SMILES

O=C(O)/C=C/C1=CC=C(/C(C2=CC3=C(NN=C3)C=C2)=C(C4=CC=C(F)C=C4Cl)/CC)C=C1
Synonyms

ARN-810; GDC-0810
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

All

Sort by:

Journal Impact Factor

Cell Rep

Carvedilol sensitizes chemotherapy by targeting STING to boost anti-tumor immunity. [Abstract]

2025 Apr 16;44(5):115572. PMID: 40249703
Mol Cancer Ther

The Dysregulated Pharmacology of Clinically Relevant ESR1 Mutants is Normalized by Ligand-activated WT Receptor. [Abstract]

2020 Jul;19(7):1395-1405. PMID: 32381587
BMC Cancer

PPP4C: a potential molecular marker and therapeutic target in thyroid cancer and triple-negative breast cancer. [Abstract]

2026 May 4;26(1):768. PMID: 42082953
Breast Cancer Res Treat

Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy. [Abstract]

2020 Jan;179(1):67-77. PMID: 31562570
Harvard University

2023 Mar. 30487357.
University of London

2022 May.
Horm Cancer

A Novel Strategy to Co-target Estrogen Receptor and Nuclear Factor κB Pathways with Hybrid Drugs for Breast Cancer Therapy. [Abstract]

2017 Jun;8(3):135-142. PMID: 28396978

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (223.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2376 mL

11.1882 mL

22.3764 mL

5 mM

0.4475 mL

2.2376 mL

4.4753 mL

10 mM

0.2238 mL

1.1188 mL

2.2376 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.65 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[1]

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)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2376 mL	11.1882 mL	22.3764 mL	55.9409 mL
	5 mM	0.4475 mL	2.2376 mL	4.4753 mL	11.1882 mL
	10 mM	0.2238 mL	1.1188 mL	2.2376 mL	5.5941 mL
	15 mM	0.1492 mL	0.7459 mL	1.4918 mL	3.7294 mL
	20 mM	0.1119 mL	0.5594 mL	1.1188 mL	2.7970 mL
	25 mM	0.0895 mL	0.4475 mL	0.8951 mL	2.2376 mL
	30 mM	0.0746 mL	0.3729 mL	0.7459 mL	1.8647 mL
	40 mM	0.0559 mL	0.2797 mL	0.5594 mL	1.3985 mL
	50 mM	0.0448 mL	0.2238 mL	0.4475 mL	1.1188 mL
	60 mM	0.0373 mL	0.1865 mL	0.3729 mL	0.9323 mL
	80 mM	0.0280 mL	0.1399 mL	0.2797 mL	0.6993 mL
	100 mM	0.0224 mL	0.1119 mL	0.2238 mL	0.5594 mL

Bioz

Keywords

Brilanestrant

7 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Brilanestrant

Fulvestrant

AZD9496

LSZ-102

Tamoxifen

GDC-0927

Elacestrant

PHTPP

Acolbifene

GSK-4716

Fulvestrant (Standard)

Camizestrant

Giredestrant

Publications Citing Use of MedChemExpress (MCE) Brilanestrant

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

Brilanestrant

Fulvestrant

AZD9496

LSZ-102

Tamoxifen

GDC-0927

Elacestrant

PHTPP

Acolbifene

GSK-4716

Fulvestrant (Standard)

Camizestrant

Giredestrant

Publications Citing Use of MedChemExpress (MCE) Brilanestrant

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Brilanestrant Related Classifications

HY-12864 Related Classifications

Bioz