ERα degrader 7
ERα degrader 7 (compound B1) is a potent ERα degrader with an IC50 of 14.6 nM and a DC50 of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research.
For research use only. We do not sell to patients.
- Formula: C28H24F4N2O3
- Molecular Weight:512.50
-
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
IC50: 14.6 nM (ERα)[1]
ERα degrader 7 (10-5-10 μM, 5 d) demonstrates antitumor activity against the breast cancer cell (IC50 = 4.21 nM) and noncytotoxicity against normal breast epithelial cell[1].
ERα degrader 7 (50-1000 nM, 5 d) shows a significant concentration-dependent degradation effect of ERα in MCF-7[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF-10 (normal breast epithelial cell)
-
Concentration:10-5-10 μM
-
Incubation Time:5 d
-
Result:Demonstrated low inhibition against MCF-10A, cell proliferation rate of each concentration are all above 80%.
-
Cell Line:MCF-7 (breast cancer cell)
-
Concentration:10-5-10 μM
-
Incubation Time:5 d
-
Result:ERα degrader 7 (10-3-10 μM) demonstrated excellent antitumor activity against the MCF-7 cell, caused an inhibition rate ranged from 60% to 75%, results were evaluated using GDC-9545 as a positive control.
-
Cell Line:MCF-7 (breast cancer cell)
-
Concentration:1, 10, 50, 100, 200, 500, 1000 nM
-
Incubation Time:5 d
-
Result:Showed a concentration-dependent degradation effect of ERα. Demonstrated a significant ERα-degradation effect (ERα expression rate < 50%) at a concentration of 50 nM, results were evaluated using GDC-9545 as a positive control.
Chemical Information
-
Molecular Weight 512.50
-
Formula C28H24F4N2O3
-
SMILES
OC(C1=CC=C(C2=CC(F)=C([C@@H]3C(NC4=CC=CC=C45)=C5C[C@@H](C)N3CC(F)(F)CO)C(F)=C2)C=C1)=O
-
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)
ERα degrader 7 Related Classifications
HY-155492 Related Classifications
Powered by Bioz