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In vitro: AZD9496 showed pmol/L equipotent binding to both ERα and ERβ isoforms. AZD9496 directly targets ERα for downregulation in vitro. And it also antagonizes and downregulates mutant ER in vitro and in vivo. The IC50s of ERα binding, ERα downregulation, ERα antagonism for AZD9496 are 0.82, 0.14 and 0.28 nM, respectively.
In vivo: AZD9496 showed high oral bioavailability across three species (F% 63, 91, and 74, rat, mouse, and dog, respectively) with generally low volume and clearance across species, albeit a higher clearance in mouse. The percent free levels in human plasma of 0.15% were 5-fold higher than those measured for fulvestrant. AZD9496 is a potent, oral inhibitor of breast tumor growth in vivo. AZD9496 causes tumor regressions in combination with PI3K pathway and CDK4/6 inhibitors and in an estrogen-deprived ER+ model of resistance. This effect was accompanied by a dose-dependent decrease in PR protein levels. AZD9496 is currently being evaluated in a phase I clinical trial.
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 cells |
| Preparation method | Cells were grown in steroid-free conditions in SILAC media containing 13C615N4 L-arginine to label ERα peptide as "heavy" and then switched to grow in media containing unlabeled l-arginine to label newly synthesized protein as "normal" with 0.1% DMSO, 300 nmol/L tamoxifen, 100 nmol/L AZD9496, or 100 nmol/L fulvestrant for the time indicated. |
| Concentrations | 100 nM |
| Incubation time | 0, 10, 20, 30, 40, 50 h |
| Animal Experiment | |
|---|---|
| Animal models | Sexually immature female Han Wistar rats |
| Formulation | PEG/Captisol |
| Dosages | 5 and 25 mg/kg once daily |
| Administration | oral gavage |
| Molecular Weight | 442.47 |
| Formula | C25H25F3N2O2 |
| CAS Number | 1639042-08-2 |
| Solubility (25°C) | 88 mg/mL in DMSO |
| Storage | 4°C, protect from light |
| Related Estrogen Receptor Products |
|---|
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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. |
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