Giredestrant
Based on 6 publication(s) in Google Scholar
Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.98%
- CAS. Nr.: 1953133-47-5
- Formel: C27H31F5N4O
- Molecular Weight:522.55
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) Giredestrant
More
Biologische Aktivität
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ER |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | EC50 |
0.4 nM
Compound: 35; GDC-9545
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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] |
Giredestrant (GDC-9545) is a novel ER antagonist that combines desirable mechanistic and pre-clinical DMPK attributes. The highly potent in vivo efficacy of Giredestrant likely arises due to the particular combination of high binding potency, full suppression of ER signaling, and an improved DMPK profile[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1953133-47-5
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Appearance Solid
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Molecular Weight 522.55
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Formel C27H31F5N4O
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Color Light yellow to yellow
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SMILES
OCC(F)(F)CN([C@@H]1C2=C(F)C=C(NC3CN(CCCF)C3)C=C2F)[C@H](C)CC4=C1NC5=C4C=CC=C5
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Synonyms
GDC-9545; RG6171
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Cancer Discov
2024 Feb 8;14(2):274-289. PMID: 37982575 -
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bioRxiv
Targeting Unique Ligand Binding Domain Structural Features Downregulates DKK1 in Y537S ESR1 Mutant Breast Cancer Cells. [Abstract]2024 Jun 2:2024.05.28.596307. PMID: 38854123 -
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Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (95.68 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. 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. 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: ≥ 2.5 mg/mL (4.78 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.78 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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. 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 | 1.9137 mL | 9.5685 mL | 19.1369 mL | 47.8423 mL |
| 5 mM | 0.3827 mL | 1.9137 mL | 3.8274 mL | 9.5685 mL | |
| 10 mM | 0.1914 mL | 0.9568 mL | 1.9137 mL | 4.7842 mL | |
| 15 mM | 0.1276 mL | 0.6379 mL | 1.2758 mL | 3.1895 mL | |
| 20 mM | 0.0957 mL | 0.4784 mL | 0.9568 mL | 2.3921 mL | |
| 25 mM | 0.0765 mL | 0.3827 mL | 0.7655 mL | 1.9137 mL | |
| 30 mM | 0.0638 mL | 0.3189 mL | 0.6379 mL | 1.5947 mL | |
| 40 mM | 0.0478 mL | 0.2392 mL | 0.4784 mL | 1.1961 mL | |
| 50 mM | 0.0383 mL | 0.1914 mL | 0.3827 mL | 0.9568 mL | |
| 60 mM | 0.0319 mL | 0.1595 mL | 0.3189 mL | 0.7974 mL | |
| 80 mM | 0.0239 mL | 0.1196 mL | 0.2392 mL | 0.5980 mL |
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