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Brilanestrant
🥰Excellent
Catalog No. T5118Cas No. 1365888-06-7
Alias RG 6046, GDC-0810, GDC0810, GDC 0810, ARN-810
Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM).
Brilanestrant
🥰Excellent
Purity: 98.71%
Catalog No. T5118Alias RG 6046, GDC-0810, GDC0810, GDC 0810, ARN-810Cas No. 1365888-06-7
Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | 45 € | In Stock | |
| 2 mg | 66 € | In Stock | |
| 5 mg | 102 € | In Stock | |
| 10 mg | 145 € | In Stock | |
| 25 mg | 259 € | In Stock | |
| 50 mg | 427 € | In Stock | |
| 100 mg | 614 € | In Stock | |
| 1 mL x 10 mM (in DMSO) | 122 € | In Stock |
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CitedSelect Batch
Purity:98.71%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM). |
| Targets&IC50 | ERα:0.7 nM |
| In vitro | Brilanestrant 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]. Brilanestrant 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 Brilanestrant shows it is a clearance molecule across species, with good bioavailability (40%-60%). Brilanestrant (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 exhibits low clearance (11 mL/min/kg) and 61% oral bioavailability. Brilanestrant (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. |
| Alias | RG 6046, GDC-0810, GDC0810, GDC 0810, ARN-810 |
| Molecular Weight | 446.9 |
| Formula | C26H20ClFN2O2 |
| Cas No. | 1365888-06-7 |
| Smiles | CC\C(=C(\c1ccc(\C=C\C(O)=O)cc1)c1ccc2[nH]ncc2c1)c1ccc(F)cc1Cl |
| Relative Density. | 1.342 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (123.07 mM)  H2O: Insoluble | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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