Fulvestrant-3-boronic acid
Based on 1 Customer Validation
Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells.
For research use only. We do not sell to patients.
- Purity : 99.7%
- CAS No.: 1853279-29-4
- Formula: C32H48BF5O4S
- Molecular Weight:634.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.0032 μM
Compound: 5; ZB716
|
Antiproliferative activity against human MCF7 cells after 5 days by coulter counter analysis
Antiproliferative activity against human MCF7 cells after 5 days by coulter counter analysis
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[PMID: 27529700] |
| MCF7 | IC50 |
0.069 μM
Compound: 5; ZB716
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Antiproliferative activity against human tamoxifen-resistant MCF7 cells after 5 days by coulter counter analysis
Antiproliferative activity against human tamoxifen-resistant MCF7 cells after 5 days by coulter counter analysis
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[PMID: 27529700] |
| T47D | IC50 |
0.0061 μM
Compound: 5; ZB716
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Antiproliferative activity against human T47D cells after 5 days by coulter counter analysis
Antiproliferative activity against human T47D cells after 5 days by coulter counter analysis
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[PMID: 27529700] |
| T47D | IC50 |
0.037 μM
Compound: 5; ZB716
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Antiproliferative activity against human tamoxifen-resistant T47D cells over-expressing PKC-alpha after 5 days by coulter counter analysis
Antiproliferative activity against human tamoxifen-resistant T47D cells over-expressing PKC-alpha after 5 days by coulter counter analysis
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[PMID: 27529700] |
| T47D | IC50 |
12.7 nM
Compound: 5; ZB716
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Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysis
Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysis
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[PMID: 27529700] |
| T47D | IC50 |
7.8 nM
Compound: 5; ZB716
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Downregulation of ER-alpha expression in human T47D cells measured after 5 days by Western blot analysis
Downregulation of ER-alpha expression in human T47D cells measured after 5 days by Western blot analysis
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[PMID: 27529700] |
In Vitro
Fulvestrant-3-boronic acid (1-27 nM, 5 d) dramatically down-regulates ERα protein expression in a dose-dependent manner in T47D and T47D/PKCα cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1853279-29-4
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Appearance Solid
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Molecular Weight 634.59
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Formula C32H48BF5O4S
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Color White to off-white
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SMILES
FC(F)(F)C(F)(F)CCCS(CCCCCCCCC[C@H]1[C@]2([H])[C@@](CC[C@]3([C@@]2([H])CC[C@@H]3O)C)([H])C4=CC=C(B(O)O)C=C4C1)=O
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Synonyms
ZB716
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
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Data Sheet (265 KB)
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SDS (563 KB)
- English - EN (563 KB)
- Français - FR (563 KB)
- Deutsch - DE (563 KB)
- Norwegian - NO (563 KB)
- Español - ES (563 KB)
- Swedish - SV (563 KB)
- Italian - IT (563 KB)
- Korean - KR (563 KB)
- Portuguese - PT (563 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fulvestrant-3-boronic acid Related Classifications
HY-137144 Related Classifications
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