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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.
| 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. |
| 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 |
| Related Estrogen Receptor Products |
|---|
| Fulvestrant
Fulvestrant is a Estrogen receptor (ER) antagonist with IC50 of 0.094 nM. Fulvestrant can also induce autophagy and apoptosis, and has anti-tumor effect. |
| LY500307
LY500307 is a potent, selective estrogen receptor beta agonist with an EC50 of 0.66 nM. |
| Calcitriol
Calcitriol is an Active metabolite of vitamin D3 that activates the vitamin D receptor. *The compound is unstable in solutions, freshly prepared is recommended |
| Tamoxifen Citrate (ICI 46474)
Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding. |
| 20-Hydroxyecdysone
20-Hydroxyecdysone (Ecdysterone, 20E) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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