| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C26H18F2O4S |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
ER degrader 5 is a potent degrader of the estrogen receptor (ER). It shows anti-proliferative activity and can be used in breast cancer research[1]. It has a molecular formula of C26H18F2O4S and a molecular weight of 464.48 g/mol.
Physical & Chemical Properties
| CAS Number | 2913192-47-7 |
|---|---|
| Molecular Formula | C26H18F2O4S |
| Molecular Weight | 464.48 g/mol |
| SMILES | O=C(C1=C(C=C(C=C1C)F)C)C(SC2=CC(F)=CC=C23)=C3OC4=CC=C(C=C4)/C=C/C(O)=O |
| Signaling Pathway | Vitamin D Related/Nuclear Receptor |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
ER degrader 5 (5 days) inhibits MCF-7 cell proliferation, with an IC50 of 55 nM[1]. In MCF-7 cells, ER degrader 5 arrests the cell cycle at the G0/G1 phase[1]. ER degrader 5 (1 nM-10 μM; 24 h) degrades the estrogen receptor (ER) in MCF-7 cells[1]. In MCF-7 cells, ER degrader 5 (1-10 μM; 24 h) sharply lowers the expression levels of GREB1, PGR, and TFF1[1].
Western Blot Analysis[1]
| Cell Line | MCF-7 cells |
|---|---|
| Concentration | 1, 10, 100, 1000, 10000 nM |
| Incubation Time | 24 hours |
| Result | Degraded ER in a dose-dependent manner. |
Real Time qPCR[1]
| Cell Line | MCF-7 cells |
|---|---|
| Concentration | 1, 5, 10 μM |
| Incubation Time | 24 hours |
| Result | Decreased the expression levels of GREB1, PGR, and TFF1 in a dose-dependent manner. |
In Vivo
In a MCF-7 xenograft model, daily i.p. dosing of ER degrader 5 at 30 mg/kg for 30 days significantly inhibits tumor growth[1]. Given i.v. at 3 mg/kg, ER degrader 5 has a half-life of 1.23 h and a Cmax of 4497 ng/mL[1]. Given p.o. at 30 mg/kg, it reaches an oral bioavailability of 62.9%[1].
| Animal Model | Female nude mice injected with MCF-7 cells[1] |
|---|---|
| Dosage | 30 mg/kg |
| Administration | I.p. daily for 30 days |
| Result | Inhibited tumor growth and observed no significant body weight loss. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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