Free shipping on all orders over $ 500

GDC-0810

Cat. No. M8953
GDC-0810 Structure
Synonym:

Brilanestrant; ARN-810

Size Price Availability Quantity
5mg USD 140  USD140 In stock
10mg USD 210  USD210 In stock
50mg USD 560  USD560 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

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.

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. 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.

Protocol (for reference only)
Cell Experiment
Cell lines MCF-7 cells
Preparation method 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).
Concentrations
Incubation time 5 days
Animal Experiment
Animal models tamoxifen-sensitive MCF-7 xenograft model
Formulation PEG400/PVP/TW80/0.5% CMC in water, 9:0.5:0.5:90
Dosages 30 and 100 mg/kg
Administration p.o.
Chemical Information
Molecular Weight 446.90
Formula C26H20ClFN2O2
CAS Number 1365888-06-7
Solubility (25°C) DMSO: ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Joseph JD, et al. Elife. The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.

[2] Lai A, et al. J Med Chem. Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.

Related Estrogen Receptor Products
hFSH-β-(33-53) TFA

hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells.

Yp537

Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor.

Palazestrant

Palazestrant is a novel, orally active, estrogen receptor antagonist and selective estrogen receptor degrader. It can be used in studies related to ER+/HER2+ breast cancer.

Acolbifene hydrochloride

Acolbifene hydrochloride is an active metabolite of EM800 and an orally available, selective estrogen receptor modulator (SERM) that inhibits estradiol-induced ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM) transcriptional activity, has significant anti-estrogenic effects on the mammary gland and uterus, and has anticancer activity. possesses anticancer activity.

Acolbifene

Acolbifene is an active metabolite of EM800 and an orally active pure anti-estrogen and selective estrogen receptor (ER) antagonist that inhibits estradiol-induced ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM) transcriptional activity and has anticancer activity.

  Catalog
Abmole Inhibitor Catalog




Keywords: GDC-0810, Brilanestrant; ARN-810 supplier, Estrogen Receptor, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.