Brilanestrant (Synonyms: ARN-810; GDC-0810)

Name: Brilanestrant
Brand: MedChemExpress
SKU: HY-12864
Rating: 5.0 (5 reviews)

Cat. No.: HY-12864 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

Brilanestrant Chemical Structure

CAS No. : 1365888-06-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 158	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 158	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 216	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 576	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 780	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE Brilanestrant

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View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms

Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

IC50: 0.7 nM (estrogen receptor)

Cellular Effect

Cell Line	Type	Value	Description	References
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	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	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	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	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	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]
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	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	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	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]

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

Molecular Weight

446.90

Formula

C₂₆H₂₀ClFN₂O₂

CAS No.

1365888-06-7

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (254 KB) LCMS (259 KB)

Handling Instructions (2659 KB)

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]

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

Complete Stock Solution Preparation Table

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

Brilanestrant Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Brilanestrant1365888-06-7ARN-810 GDC-0810ARN810ARN 810GDC0810GDC 0810GDC-0810Estrogen Receptor/ERRInhibitorinhibitorinhibit

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Brilanestrant (Synonyms: ARN-810; GDC-0810)

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Brilanestrant Related Antibodies

5 Publications Citing Use of MCE Brilanestrant

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•Related Small Molecules:

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View All Estrogen Receptor/ERR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Brilanestrant Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Brilanestrant Related Classifications

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