Edotreotide
Based on 2 publication(s) in Google Scholar
Edotreotide is a ligand that selectively targets SSTR2 and can competitively bind to the receptor. Edotreotide mediates the targeted delivery, while modificated with radionuclides (such as 90Y, 177Lu, and 68Ga) to SSTR-positive tumors and induces tumor cell apoptosis by releasing β rays. Edotreotide has strong tumor targeting and precise killing activity. Edotreotide is used in the synthesis of radionuclide-drug conjugates (RDCs) and is widely used in the field of neuroendocrine tumors (such as metastatic carcinoids, lung and thymus NETs).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.71%
- CAS. Nr.: 204318-14-9
- Formel: C65H92N14O18S2
- Molecular Weight:1421.64
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Speicherung:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Edotreotide
MoreAlle Radionuclide-Drug Conjugates (RDCs) Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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Other |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
393 nM
Compound: DOTA-TOC
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In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=6)
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=6)
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[PMID: 15828816] |
| CHO-K1 | IC50 |
>10000 nM
Compound: DOTA-TOC
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In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 1 expressed in CHO-K1 cells; (n=7)
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 1 expressed in CHO-K1 cells; (n=7)
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[PMID: 15828816] |
177Edotreotide may significantly prolong progression-free survival (PFS) in lung cancer NET and TC compared with Everolimus (HY-10218) in thymic neuroendocrine applications[3].
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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CAS. Nr. 204318-14-9
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Appearance Solid
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Molecular Weight 1421.64
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Formel C65H92N14O18S2
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Color White to off-white
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Synonyms
DOTATOC; SDZ-SMT 487; SMT 487
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Pharmaceuticals (Basel)
2025 Aug 26;18(9):1274. PMID: 41011146 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (70.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 5 mg/mL (3.52 mM; ultrasonic and warming and heat to 60°C)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 2.5 mg/mL (1.76 mM); Clear solution; Need ultrasonic
Reinheit & Dokumentation
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Data Sheet (280 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
[1]. Bushnell DL Jr, et al. 90Y-edotreotide for metastatic carcinoid refractory to octreotide. J Clin Oncol. 2010 Apr 1;28(10):1652-9. [Content Brief]
[2]. Gallicchio R, et al. Ga-68-Edotreotide Positron Emission Tomography/Computed Tomography Somatostatin Receptors Tumor Volume Predicts Outcome in Patients With Primary Gastroenteropancreatic Neuroendocrine Tumors. Cancer Control. 2023 Jan-Dec;30:10732748231152328. [Content Brief]
[3]. Capdevila J, et al. A Randomized clinical trial evaluating the impact on survival and quality of life of 177Lutetium[Lu]-edotreotide versus everolimus in patients with neuroendocrine tumors of the lung and thymus: the LEVEL study (GETNE T-2217). BMC Cancer. 2025 Apr 4;25(1):613. [Content Brief]
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.7034 mL | 3.5171 mL | 7.0341 mL | 17.5853 mL |
| DMSO | 5 mM | 0.1407 mL | 0.7034 mL | 1.4068 mL | 3.5171 mL |
| 10 mM | 0.0703 mL | 0.3517 mL | 0.7034 mL | 1.7585 mL | |
| 15 mM | 0.0469 mL | 0.2345 mL | 0.4689 mL | 1.1724 mL | |
| 20 mM | 0.0352 mL | 0.1759 mL | 0.3517 mL | 0.8793 mL | |
| 25 mM | 0.0281 mL | 0.1407 mL | 0.2814 mL | 0.7034 mL | |
| 30 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5862 mL | |
| 40 mM | 0.0176 mL | 0.0879 mL | 0.1759 mL | 0.4396 mL | |
| 50 mM | 0.0141 mL | 0.0703 mL | 0.1407 mL | 0.3517 mL | |
| 60 mM | 0.0117 mL | 0.0586 mL | 0.1172 mL | 0.2931 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Edotreotide Related Classifications
HY-106033 Related Classifications
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