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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 |
|---|
| GDC-0927
GDC-0927 (SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist. |
| AC-186
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. |
| Idoxifene
Idoxifene (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM). |
| (R)-Equol
(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively. |
| (Rac)-Vepdegestrant
(Rac)-Vepdegestrant is the isomer of Vepdegestrant. |
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