PROTAC ERα Degrader-9
PROTAC ERα Degrader-9 is a dual-target degrader of estrogen receptor α (ERα) and aromatase (ARO/CYP19A), with a Ki value of 0.25 μM against human ERα and an IC50 value of 4.6 μM against human ARO. PROTAC ERα Degrader-9 degrades ERα and ARO via the ubiquitin-proteasome system, and inhibits the transcriptional activity of ERα and the enzymatic activity of ARO. PROTAC ERα Degrader-9 selectively inhibits cancer cell proliferation, induces cell cycle arrest, and triggers apoptosis. PROTAC ERα Degrader-9 exhibits antiproliferative activity and ERα-degrading activity against cancer cells carrying ERα mutations. PROTAC ERα Degrader-9 can be used in cancer-related research such as breast cancer.
(Pink: ERα and Aromatase ligand (HY-163680); Blue: VHL ligand (HY-112078); Black: linker (HY-W007559)).
For research use only. We do not sell to patients.
- Formula: C58H64F3N7O9S2
- Molecular Weight:1124.30
-
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
All PROTACs Isoforms
More
Biological Activity
|
ERα 0.25 μM (Ki) |
Aromatase 4.6 μM (IC50) |
PROTAC ERα Degrader-9 (compound 18c) preferentially binds to human ERα over ERβ, with an ERα Ki of 0.25 μM and an α/β selectivity ratio > 291; it inhibits the activity of recombinant human aromatase with an IC50 of 4.6 μM[1].
PROTAC ERα Degrader-9 (5 μM plus 10 nM Estradiol (HY-B0141); 24 h) acts as an ERα antagonist in HEK-293T cells and inhibits estradiol-induced ERα-responsive luciferase activity[1].
PROTAC ERα Degrader-9 (96 h) potently inhibits the proliferation of MCF-7, MCF-7Y537S, MCF-7D538G and MCF-7EGFR breast cancer cells, with IC50 values of 0.54 μM, 2.3 μM, 0.31 μM and 0.075 μM, respectively, and exhibits low toxicity against normal MCF-10A breast cells[1].
PROTAC ERα Degrader-9 (0.1-10 μM; 24 h) induces concentration-dependent proteasome-mediated degradation of ERα and ARO proteins in MCF-7, MCF-7D538G and MCF-7EGFR breast cancer cells, and induces potent ERα degradation with reduced ARO degradation in MCF-7Y537S cells[1].
PROTAC ERα Degrader-9 (0.5-5 μM) inhibits colony formation of MCF-7Y537S, MCF-7D538G and MCF-7EGFR ERα-mutant breast cancer cells[1].
PROTAC ERα Degrader-9 (5 μM) downregulates the mRNA expression levels of ESR1 and MYC in MCF-7, MCF-7Y537S, MCF-7D538G and MCF-7EGFR breast cancer cells[1].
PROTAC ERα Degrader-9 (5 μM; 48 h) induces G2/M phase cell cycle arrest in MCF-7 breast cancer cells[1].
PROTAC ERα Degrader-9 (1-10 μM; 48 h) induces concentration-dependent apoptosis and cell death in MCF-7 breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF-7, MCF-7Y537S, MCF-7D538G, and MCF-7EGFR breast cancer cells
-
Concentration:0.1, 0.5, 1, 5, 10 μM
1 μM (cotreated with 5 μM MG132 (HY-13259)) -
Incubation Time:24 h
-
Result:Significantly reduced ERα and ARO protein levels in MCF-7 cells at 1 μM for 24 h.
Showed concentration-dependent degradation of both proteins, with decreasing compound concentrations correlating with increasing remaining protein levels.
Cotreatment with the proteasome inhibitor MG132 blocked degradation of ERα and ARO, confirming proteasome-dependent activity.
Effectively degraded both ERα and ARO in MCF-7D538G and MCF7EGFR cells (concentration-dependent), and showed superior ERα degradation with lower ARO degradation activity in MCF7Y537S cells.
-
Cell Line:MCF-7 breast cancer cells
-
Concentration:5 μM
-
Incubation Time:48 h
-
Result:Increased the percentage of MCF-7 cells in the G2/M phase from 54.10% to 66.31%, inducing G2/M cell cycle arrest.
-
Cell Line:MCF-7 breast cancer cells
-
Concentration:1, 5, 10 μM
-
Incubation Time:48 h
-
Result:Induced MCF-7 cell death and apoptosis in a concentration-dependent manner, with higher concentrations leading to increased proportions of dead and apoptotic cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Balb/c nude (female, 4 weeks old, subcutaneous xenograft model via injection of 1 × 107 MCF-7 cells)[1]
-
Dosage:5 mg/kg
-
Administration:i.p.; every other day
-
Result:Achieved significant tumor growth inhibition, with final tumor weights and volumes notably lower than the control group.
Reduced ERα and ARO protein levels in tumor tissue significantly compared to the control group.
Lowered the number of Ki67-positive tumor cells, indicating suppressed tumor cell proliferation.
Caused no weight loss in treated mice during the study.
Showed normal cellular morphology in heart, liver, spleen, and kidney tissues via H&E staining.
Chemical Information
-
Molecular Weight 1124.30
-
Formula C58H64F3N7O9S2
-
SMILES
OC1=CC=C(C2=C([C@@H]3C(C[C@H]2O3)S(N(CC(F)(F)F)C4=CC=C(C=C4)OCCCCCC(N[C@H](C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C=C6)C7=C(N=CS7)C)C)=O)=O)C(C)(C)C)=O)(=O)=O)C8=CC=C(C=C8)N9C=CN=C9)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)
PROTAC ERα Degrader-9 Related Classifications
HY-163679 Related Classifications
Powered by Bioz