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SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation. SAR439859 has demonstrated broader and superior ER antagonist and degrader activities across a large panel of ER+ cells, including inhibition of ER signaling and tumor cell growth.
In vivo treatment with SAR439859 demonstrates significant tumor regression in ER+ breast cancer models, including MCF7-ESR1 wild-type and mutant-Y537S mouse tumors, and HCI013, a patient-derived tamoxifen-resistant xenograft tumor. SAR439859 (2.5-25 mg/kg; orally twice daily for 30 days) exhibits substantial tumor-growth inhibition and displays tumor regression at the dose of 25 mg/kg/BID.
| Cell Experiment | |
|---|---|
| Cell lines | LCC2 cells, MCF7 cells |
| Preparation method | Trypsinized cells are dispensed into 384-well plates in IMEM (supplemented with 5% FBS) and after overnight incubation cells are treated with SAR439859 for the times indicated. Cell viability is assessed using CellTiter-Glo according to the manufacturer’s protocol and relative luminescence units (RLU) are measured using an Envision Multilabel Reader. The RLUs of the treated samples are normalized to that of the untreated samples and cell viability is expressed as a percentage of the value of the untreated cells. |
| Concentrations | 0.01-1000 nM |
| Incubation time | 7 days, 4 hours |
| Animal Experiment | |
|---|---|
| Animal models | Nu/nu mouse with MCF7 tumor xenograft model |
| Formulation | solution (0.6 mg/mL) in glycofurol/PS80/G5 (10%/5%/85%) and solution (1 mg/mL) in labrasol/solutol/G5 (20%/5%/75%) |
| Dosages | 2.5, 5, 12.5, 25 mg/kg |
| Administration | Orally; twice daily for 30 days |
| Molecular Weight | 554.48 |
| Formula | C31H30Cl2FNO3 |
| CAS Number | 2114339-57-8 |
| Solubility (25°C) | DMSO 80 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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