GNE-274
Based on 1 Customer Validation
GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
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- Reinheit: 98.00%
- CAS. Nr.: 2369048-69-9
- Formel: C29H31NO4
- Molecular Weight:457.56
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Speicherung:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
GNE-274 (0.1 nM-1000 nM; 4 hours) fails to trigger increased ER turnover in MCF7, MD-134, HCC1500 and CAMA cells[1].GNE-274 (1-1000 nM; 7-10 days) potently inhibits cellular proliferation, exhibiting greater potency than fulvestrant, 4-OHT, AZD9496, and GDC-0810 in E2-stimulated ER+ breast cancer cell lines[1].In transposaseaccessible chromatin sequencing (ATAC-seq) assay, GNE-274 increase chromatin accessibility at ER-DNA binding sites, it significantly alters chromatin accessibility at 594 sites. But GDC-0927 has considerably less impact on chromatin accessibility[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7, MB-134, HCC1500, EFM-19, CAMA-1, T-47D cells
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Concentration:1 nM; 10 nM; 100 nM; 1000 nM
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Incubation Time:7-10 days
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Result:Exhibited IC50 values approximately ranging from 5nM to 20 nM in different cells.
Chemical Information
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CAS. Nr. 2369048-69-9
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Appearance Solid
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Molecular Weight 457.56
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Formel C29H31NO4
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Color Off-white to light yellow
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SMILES
CCCN1CC(C1)COC2=CC=C([C@@H]3OC4=CC=C(C=C4C(C)=C3C5=CC(O)=CC=C5)O)C=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Lösungsmittel & Löslichkeit
DMSO : 200 mg/mL (437.10 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: 1.75 mg/mL (3.82 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1.75 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.5 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: 1.75 mg/mL (3.82 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1.75 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.5 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1855 mL | 10.9275 mL | 21.8551 mL | 54.6376 mL |
| 5 mM | 0.4371 mL | 2.1855 mL | 4.3710 mL | 10.9275 mL | |
| 10 mM | 0.2186 mL | 1.0928 mL | 2.1855 mL | 5.4638 mL | |
| 15 mM | 0.1457 mL | 0.7285 mL | 1.4570 mL | 3.6425 mL | |
| 20 mM | 0.1093 mL | 0.5464 mL | 1.0928 mL | 2.7319 mL | |
| 25 mM | 0.0874 mL | 0.4371 mL | 0.8742 mL | 2.1855 mL | |
| 30 mM | 0.0729 mL | 0.3643 mL | 0.7285 mL | 1.8213 mL | |
| 40 mM | 0.0546 mL | 0.2732 mL | 0.5464 mL | 1.3659 mL | |
| 50 mM | 0.0437 mL | 0.2186 mL | 0.4371 mL | 1.0928 mL | |
| 60 mM | 0.0364 mL | 0.1821 mL | 0.3643 mL | 0.9106 mL | |
| 80 mM | 0.0273 mL | 0.1366 mL | 0.2732 mL | 0.6830 mL | |
| 100 mM | 0.0219 mL | 0.1093 mL | 0.2186 mL | 0.5464 mL |
GNE-274 Related Classifications
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