GNE-149
Based on 1 Customer Validation
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.
For research use only. We do not sell to patients.
- Purity: 99.18%
- CAS No.: 1953132-75-6
- Formula: C28H33F4N3O
- Molecular Weight:503.57
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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ERα 0.053 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | EC50 |
0.7 nM
Compound: 13; GNE-149
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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 | IC50 |
0.053 nM
Compound: 12; GNE-149
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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 |
0.66 nM
Compound: 1 (GNE-149)
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Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured by CellTiter-Glo luminescent assay assay
Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured by CellTiter-Glo luminescent assay assay
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[PMID: 34425201] |
| MCF7 | IC50 |
0.66 nM
Compound: 12; GNE-149
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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 |
0.031 nM
Compound: 12; GNE-149
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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] |
| T47D | IC50 |
0.69 nM
Compound: 12; GNE-149
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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] |
GNE-149 exhibits antiproliferative activity in MCF7 and T47D cells with IC50s of 0.66 and 0.69 nM, respectively[1].
GNE-149 exhibits ERα Degradation in MCF7 and T47D cells with IC50s of 0.053 and 0.031 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GNE-149 has favorable pharmacokinetic profile, including total clearance (CL; 19, 8, and 13 mL/min/kg for Rat, Dog, and Cyno) and oral bioavailability (F; 31%, 49%, and 28% for Rat, Dog, and Cyno)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Crl:NU Foxn1 nu mice (at 7 weeks of age) bearing wild-type (WT) ERαor overexpressed Y537S mutant MCF7 tumor[1]
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Dosage:0.3, 1, 3, 10, and 30 mg/kg
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Administration:Orally q.d. for 21 days
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Result:Exhibited dose-dependent efficacy in the MCF7 WT and Y537S mutant xenograft model, with tumor regression observed at all doses above 0.3 mg/kg in Y537S mutant xenograft model.
Chemical Information
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CAS No. 1953132-75-6
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Appearance Solid
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Molecular Weight 503.57
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Formula C28H33F4N3O
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Color White to light yellow
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SMILES
CC(C)(F)CN1[C@@](C2=C(C=C(C=C2F)OC3CN(C3)CCCF)F)([H])C4=C(C[C@H]1C)C5=CC=CC=C5N4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 50 mg/mL (99.29 mM; ultrasonic and warming and heat to 60°C; 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). 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 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)
References
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). 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 | 1.9858 mL | 9.9291 mL | 19.8582 mL | 49.6455 mL |
| 5 mM | 0.3972 mL | 1.9858 mL | 3.9716 mL | 9.9291 mL | |
| 10 mM | 0.1986 mL | 0.9929 mL | 1.9858 mL | 4.9646 mL | |
| 15 mM | 0.1324 mL | 0.6619 mL | 1.3239 mL | 3.3097 mL | |
| 20 mM | 0.0993 mL | 0.4965 mL | 0.9929 mL | 2.4823 mL | |
| 25 mM | 0.0794 mL | 0.3972 mL | 0.7943 mL | 1.9858 mL | |
| 30 mM | 0.0662 mL | 0.3310 mL | 0.6619 mL | 1.6549 mL | |
| 40 mM | 0.0496 mL | 0.2482 mL | 0.4965 mL | 1.2411 mL | |
| 50 mM | 0.0397 mL | 0.1986 mL | 0.3972 mL | 0.9929 mL | |
| 60 mM | 0.0331 mL | 0.1655 mL | 0.3310 mL | 0.8274 mL | |
| 80 mM | 0.0248 mL | 0.1241 mL | 0.2482 mL | 0.6206 mL |
GNE-149 Related Classifications
HY-145341 Related Classifications
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