ERα/RAD51 degrader 1
ERα/RAD51 degrader 1 is a ERα and RAD51 HyT degrader as well as an apoptosis (Apoptosis) inducer. ERα/RAD51 degrader 1 induces conformational changes in helices 11-12 of ERα, promotes the recruitment of Hsp70, and drives the degradation of ERα and RAD51 via the ubiquitin-proteasome pathway. ERα/RAD51 degrader 1 downregulates the expression of BRCA1/2. ERα/RAD51 degrader 1 acts on tamoxifen (HY-13757A)-sensitive and tamoxifen-resistant breast cancer in both in vitro and in vivo models. ERα/RAD51 degrader 1 is applicable to breast cancer-related research (hydrophobic tag: (HY-B0402)).
For research use only. We do not sell to patients.
- Formula: C39H41F3N2O7S
- Molecular Weight:738.81
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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]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HSP70 |
ERα |
ERα/RAD51 degrader 1 (Compound 20a) inhibits the viability of LCC2 cells after 72 h, with an IC50 value of 7.727 μM[1].
ERα/RAD51 degrader 1 (0.5-15 μM; 3-48 h) induces dose- and time-dependent proteasomal degradation of ERα in MCF-7, T47D and LCC2 breast cancer cells, a process driven by Hsp70-mediated ubiquitination[1].
ERα/RAD51 degrader 1 (1-10 μM; 24 h) induces G1-phase cell cycle arrest in Tamoxifen (HY-13757A)-resistant LCC2 breast cancer cells[1].
ERα/RAD51 degrader 1 (1-20 μM; 48-72 h) induces apoptosis in MCF-7, T47D, and tamoxifen-resistant LCC2 breast cancer cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, T47D, LCC2
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Concentration:1-10 μM
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Incubation Time:24 h
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Result:Increased G1 phase proportion from 66.0% (control) to 79.3% (10 μM), while reducing S phase proportion.
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Cell Line:MCF-7, T47D, LCC2
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Concentration:1-20 μM
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Incubation Time:72 h (flow cytometry); 48 h (Western blot)
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Result:Dose-dependently increased apoptosis in MCF-7 cells.
Dose-dependently increased apoptosis in T47D cells.
Increased apoptosis in LCC2 cells.
| Species | Dose | Route | Bioavailability |
|---|---|---|---|
| Rat[1] | 5 mg/kg | i.p. | 33 % |
ERα/RAD51 degrader 1 (2.5-5 mg/kg; i.p.; once every 2 days) inhibits tumor growth of LCC2 breast cancer xenografts, with the 5 mg/kg dose exhibiting superior efficacy to Fulvestrant and no organ toxicity observed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 4-week-old, subcutaneous xenograft of MCF-7 cells, estradiol valerate supplementation)[1]
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Dosage:5 mg/kg
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Administration:i.p.; every 2 days
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Result:Reduced tumor volume and weight more effectively than fulvestrant.
Reduced Ki67 (cell proliferation marker) in tumor tissues.
Showed no significant abnormalities or damage in heart, liver, spleen, and kidney tissues via H&E staining.
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Animal Model:BALB/c nude (female, 4-week-old, subcutaneous xenograft of tamoxifen-resistant LCC2 cells, estradiol valerate supplementation)[1]
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Dosage:2.5 mg/kg; 5 mg/kg
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Administration:i.p.; every 2 days
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Result:Effectively inhibited tumor growth at both 2.5 mg/kg and 5 mg/kg doses.
Outperformed fulvestrant at the 5 mg/kg dose.
Reduced Ki67 (cell proliferation marker) in tumor tissues.
Showed no significant abnormalities or damage in heart, liver, and kidney tissues via H&E staining.
Chemical Information
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Molecular Weight 738.81
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Formula C39H41F3N2O7S
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SMILES
O=S(N(C1=CC=C(C=C1)OCCC(NC23C[C@H](C[C@@H](C4)C3)C[C@H]4C2)=O)CC(F)(F)F)(C5C[C@@H]6C(C7=CC=C(O)C=C7)=C(C8=CC=C(O)C=C8)[C@H]5O6)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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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/RAD51 degrader 1 Related Classifications
HY-187096 Related Classifications
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