GDC-0927
Based on 3 publication(s) in Google Scholar
GDC-0927 (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.98%
- No. CAS: 1642297-01-5
- Fòrmula: C28H28FNO4
- Peso molecular:461.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GDC-0927
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Actividad biológica
Estrogen receptor[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | EC50 |
0.3 nM
Compound: 11; GDC-0927
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Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay
Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay
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[PMID: 34251202] |
| MCF7 | EC50 |
0.3 nM
Compound: 3; GDC-0927
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Antiproliferative activity against human MCF7 cells after 72 hrs by Celltiter-Glo assay
Antiproliferative activity against human MCF7 cells after 72 hrs by Celltiter-Glo assay
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[PMID: 31311734] |
| MCF7 | IC50 |
0.03 nM
Compound: 3; GDC-0927
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Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst 33342 staining based immunofluorescence imaging analysis
Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst 33342 staining based immunofluorescence imaging analysis
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[PMID: 31311734] |
| MCF7 | IC50 |
0.03 nM
Compound: 5; GDC-0927
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Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis
Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis
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[PMID: 32551022] |
| MCF7 | IC50 |
0.03 nM
Compound: GDC-0927; 4
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Induction of ERalpha degradation in human MCF7 cells after 4 hrs by Alexafluor-488 conjugate anti-mouse IgG antibody/Hoechst 33342 staining based immunofluorescence imaging analysis
Induction of ERalpha degradation in human MCF7 cells after 4 hrs by Alexafluor-488 conjugate anti-mouse IgG antibody/Hoechst 33342 staining based immunofluorescence imaging analysis
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[PMID: 30732944] |
| MCF7 | IC50 |
0.1 nM
Compound: 17ha; GDC-0927; SRN-927
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Antiproliferative activity against human MCF7 cells after 5 days by CellTiter-Glo assay
Antiproliferative activity against human MCF7 cells after 5 days by CellTiter-Glo assay
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[PMID: 30655946] |
| MCF7 | IC50 |
0.1 nM
Compound: 17ha; GDC-0927; SRN-927
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Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha protein level after 4 hrs by InCell Western assay
Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha protein level after 4 hrs by InCell Western assay
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[PMID: 30655946] |
| MCF7 | IC50 |
0.2 nM
Compound: GDC-0927; 4
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Antiproliferative activity against human MCF7 cells after 3 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human MCF7 cells after 3 days by CellTiter-Glo luminescent cell viability assay
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[PMID: 30732944] |
| MCF7 | IC50 |
0.3 nM
Compound: 5; GDC-0927
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by Celltiter-Glo assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by Celltiter-Glo assay
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[PMID: 32551022] |
| T47D | IC50 |
0.29 nM
Compound: 5; GDC-0927
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Antiproliferative activity against human T47D cells assessed as reduction in cell viability
Antiproliferative activity against human T47D cells assessed as reduction in cell viability
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[PMID: 32551022] |
| T47D | IC50 |
0.38 nM
Compound: 5; GDC-0927
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Induction of ERalpha degradation in human T47D cells
Induction of ERalpha degradation in human T47D cells
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[PMID: 32551022] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1642297-01-5
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Appearance Solid
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Peso molecular 461.52
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Fòrmula C28H28FNO4
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Color Light yellow to yellow
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SMILES
OC1=CC=C2C(C(C)=C(C3=CC=CC(O)=C3)[C@H](C4=CC=C(OCCN5CC(CF)C5)C=C4)O2)=C1
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Synonyms
SRN-927
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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J Biol Chem
The AF-2 cofactor binding region is key for the selective SUMOylation of estrogen receptor alpha by antiestrogens. [Abstract]2023 Jan;299(1):102757. PMID: 36460099 -
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Solvente y solubilidad
DMSO : 83.33 mg/mL (180.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1668 mL | 10.8338 mL | 21.6675 mL | 54.1688 mL |
| 5 mM | 0.4334 mL | 2.1668 mL | 4.3335 mL | 10.8338 mL | |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1668 mL | 5.4169 mL | |
| 15 mM | 0.1445 mL | 0.7223 mL | 1.4445 mL | 3.6113 mL | |
| 20 mM | 0.1083 mL | 0.5417 mL | 1.0834 mL | 2.7084 mL | |
| 25 mM | 0.0867 mL | 0.4334 mL | 0.8667 mL | 2.1668 mL | |
| 30 mM | 0.0722 mL | 0.3611 mL | 0.7223 mL | 1.8056 mL | |
| 40 mM | 0.0542 mL | 0.2708 mL | 0.5417 mL | 1.3542 mL | |
| 50 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 1.0834 mL | |
| 60 mM | 0.0361 mL | 0.1806 mL | 0.3611 mL | 0.9028 mL | |
| 80 mM | 0.0271 mL | 0.1354 mL | 0.2708 mL | 0.6771 mL | |
| 100 mM | 0.0217 mL | 0.1083 mL | 0.2167 mL | 0.5417 mL |
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