| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C33H31F4N3O5SSe |
| SMILES | |
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Compound Overview
ER degrader 7 is a degrader of estrogen receptor α (ERα) and an inhibitor of tubulin. It reduces the viability of various cancer cell lines and disrupts the microtubule network in breast cancer cells, inducing G2/M phase cell cycle arrest and showing concentration-dependent accumulation in Tamoxifen-resistant LCC2 cells. It suppresses tumor growth in vivo without causing body weight loss and can be applied to breast cancer studies[1]. It has a molecular formula of C33H31F4N3O5SSe and a molecular weight of 736.63 g/mol.
Physical & Chemical Properties
| CAS Number | 2922929-63-1 |
|---|---|
| Molecular Formula | C33H31F4N3O5SSe |
| Molecular Weight | 736.63 g/mol |
| SMILES | O=C(CCCCC[Se]C#N)NC1=CC=C(C2=C(C3=CC=C(O)C=C3)[C@H]4CC(S(N(CC(F)(F)F)C5=C(F)C=CC=C5)(=O)=O)[C@@H]2O4)C=C1 |
| Signaling Pathway | Vitamin D Related/Nuclear Receptor; Cytoskeleton; Cell Cycle/DNA Damage |
| 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 7 potently inhibits the proliferation of the ERα-positive breast cancer cells MCF-7 and T47D, with IC50 values of 0.06 μM and 2.56 μM, respectively; compared with normal MCF-10A breast cells, it shows high cancer cell selectivity, with a selectivity index (SI) value of 264.00[1]. In the endocrine-resistant ERα-positive breast cancer cell lines LCC2, T47D538G and T47DY537S, ER degrader 7 potently inhibits proliferation, with IC50 values of 1.59 μM, 1.67 μM and 1.37 μM, respectively[1]. ER degrader 7 inhibits proliferation of the ERα-negative MDA-MB-231 breast cancer cells with an IC50 of 3.75 μM[1]. In MCF-7 cells, ER degrader 7 (0.5-5 μM; 6-24) induces proteasome-dependent ERα degradation in a dose-dependent manner, with activity comparable to that of Fulvestrant[1]. In three ERα+ drug-resistant breast cancer cell lines, ER degrader 7 (0.5-5 μM; 6-24 h) shows weak degradation activity[1]. In MCF-7 and LCC2 breast cancer cells, ER degrader 7 (2-4 μM; 48 h) disrupts the microtubule network, causing fragmentation and disorganization of microtubule structures, similar to the effect of Colchicine treatment[1]. ER degrader 7 (1-12 μM; 48 h) induces G2/M phase arrest in MCF-7 and LCC2 cells, and LCC2 cells show concentration-dependent accumulation in the G2/M phase[1]. In a competitive fluorescent receptor binding assay, ER degrader 7 binds selectively to ERα over ERβ, with an ERα RBA of 8.57%[1]. In a cell-free assay, ER degrader 7 (30 μM) significantly inhibits tubulin polymerization, with activity comparable to that of Colchicine[1].
Western Blot Analysis[1]
| Cell Line | MCF-7 cells |
|---|---|
| Concentration | 0.5, 1 and 5 μM |
| Incubation Time | 6, 12 and 24 h |
| Result | Induced ERα degradation in a concentration-dependent manner. Exhibited good degradation activity at 1 μM, comparable to that of Fulvestrant. |
Immunofluorescence[1]
| Cell Line | MCF-7 and LCC2 breast cancer cells |
|---|---|
| Concentration | 2 μM (MCF-7 cells); 4 μM (LCC2 cells) |
| Incubation Time | 48 h |
| Result | Disrupted microtubule networks in MCF-7 and LCC2 breast cancer cells, causing microtubule fragmentation and disorganization, similar to the effect observed with Colchicine treatment. |
Cell Cycle Analysis[1]
| Cell Line | MCF-7 and LCC2 breast cancer cells |
|---|---|
| Concentration | 1, 4 and 8 μM (MCF-7 cells); 3, 6 and 12 μM (LCC2 cells) |
| Incubation Time | 48 h |
| Result | Induced G2/M phase arrest in MCF-7 and LCC2 cells, with the percentage of MCF-7 cells at G2/M increasing from 17.45% to 40.88%, and LCC2 cells showing a concentration-dependent accumulation in G2/M phase. |
In Vivo
Tumor growth is inhibited by ER degrader 7 at 2-4 mg/kg (i.p.; once every two days) in nude mouse xenograft models of MCF-7 and tamoxifen-resistant LCC2. No body weight loss is caused over the course of treatment, and ERα degradation with reduced Ki67 positivity accompanies this in tumor tissues[1].
| Animal Model | Nude mice were subcutaneously inoculated with MCF-7 cells and Tamoxifen-resistant LCC2 cells to establish an ERα+ breast cancer xenograft mode[1] |
|---|---|
| Dosage | 2 and 4 mg/kg |
| Administration | i.p.; once every two days |
| Result | Achieved tumor growth inhibition (TGI) of 51.39% at 2 mg/kg, without body-weight loss, accompanied by tumor-tissue ERα degradation and reduced Ki67 positivity[. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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