ER degrader 7
ER degrader 7 is an estrogen receptor α (ERα) degrader and a tubulin (tubulin) inhibitor. ER degrader 7 inhibits the cell viability of various cancer cell lines. ER degrader 7 disrupts the microtubule network in breast cancer cells, induces G2/M phase cell cycle arrest, and exhibits concentration-dependent accumulation in Tamoxifen-resistant LCC2 cells. ER degrader 7 suppresses tumor growth in vivo without causing body weight loss. ER degrader 7 can be applied in studies related to breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2922929-63-1
- Formula: C33H31F4N3O5SSe
- Molecular Weight:736.63
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.06 μM
|
Antiproliferative activity against human MCF-7 ERα-positive breast cancer cells assessed as reduction in cell viability.
Antiproliferative activity against human MCF-7 ERα-positive breast cancer cells assessed as reduction in cell viability.
|
37584263 |
| T47D | IC50 |
2.56 μM
|
Antiproliferative activity against human T47D ERα-positive breast cancer cells assessed as reduction in cell viability.
Antiproliferative activity against human T47D ERα-positive breast cancer cells assessed as reduction in cell viability.
|
37584263 |
| MCF-10A | IC50 |
15.84 μM
|
Cytotoxicity against human MCF-10A normal breast cells assessed as reduction in cell viability.
Cytotoxicity against human MCF-10A normal breast cells assessed as reduction in cell viability.
|
37584263 |
| MDA-MB-231 | IC50 |
3.75 μM
|
Antiproliferative activity against human MDA-MB-231 ERα-negative breast cancer cells assessed as reduction in cell viability.
Antiproliferative activity against human MDA-MB-231 ERα-negative breast cancer cells assessed as reduction in cell viability.
|
37584263 |
In Vitro
ER degrader 7 (compound 35t) potently inhibits the proliferation of MCF-7 and T47D ERα-positive breast cancer cells, with IC50 values of 0.06 μM and 2.56 μM, respectively; it exhibits high cancer cell selectivity compared to normal MCF-10A breast cells, with a selectivity index (SI) value of 264.00[1].
ER degrader 7 potently inhibits the proliferation of endocrine-resistant ERα-positive breast cancer cell lines LCC2, T47D538G and T47DY537S, with IC50 values of 1.59 μM, 1.67 μM and 1.37 μM, respectively[1].
ER degrader 7 inhibits the proliferation of ERα-negative MDA-MB-231 breast cancer cells with an IC50 of 3.75 μM[1].
ER degrader 7 (0.5-5 μM; 6-24) induces proteasome-dependent ERα degradation in a dose-dependent manner in MCF-7 cells, with activity comparable to that of Fulvestrant (HY-13636)[1].
ER degrader 7 (0.5-5 μM; 6-24 h) exhibits weak degradation activity in three ERα+ drug-resistant breast cancer cell lines[1].
ER degrader 7 (2-4 μM; 48 h) disrupts the microtubule network in MCF-7 and LCC2 breast cancer cells, causing fragmentation and disorganization of microtubule structures, an effect similar to that induced by Colchicine treatment[1].
ER degrader 7 (1-12 μM; 48 h) induces G2/M phase arrest in MCF-7 and LCC2 cells, with LCC2 cells showing a concentration-dependent accumulation in the G2/M phase[1].
ER degrader 7 exhibits selective binding to ERα over ERβ, with an ERα RBA of 8.57% in a competitive fluorescent receptor binding assay[1].
ER degrader 7 (30 μM) significantly inhibits tubulin polymerization in a cell-free assay, with activity comparable to that of Colchicine (HY-16569) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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.
-
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 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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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[.
Chemical Information
-
CAS No. 2922929-63-1
-
Molecular Weight 736.63
-
Formula C33H31F4N3O5SSe
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ER degrader 7 Related Classifications
HY-155197 Related Classifications
Powered by Bioz