Vipivotide tetraxetan
Based on 17 publication(s) in Google Scholar
Vipivotide tetraxetan (PSMA-617) is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM. Vipivotide tetraxetan (PSMA-617) is designed consisting of three components: the pharmacophore Glutamate-urea-Lysine, the chelator DOTA able to complex both 68Ga or 177Lu, and a linker connecting these two entities. Glutamate-urea-Lysine is the selective pharmacophore to bind to prostate specific membrane antigen.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.46%
- CAS 番号: 1702967-37-0
- 分子式: C49H71N9O16
- 分子量:1042.14
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Vipivotide tetraxetan
More- Biosens Bioelectron. 2024 Mar 1:247:115956. [Abstract]
- J Nucl Med. 2025 Apr 1;66(4):599-604. [Abstract]
- Eur J Nucl Med Mol Imaging. 2025 Apr;52(5):1671-1684. [Abstract]
- Eur J Nucl Med Mol Imaging. 2023 Jul;50(8):2342-2352. [Abstract]
- Int J Radiat Oncol Biol Phys. 2024 Apr 1;118(5):1575-1584. [Abstract]
- Pharmaceutics. 2022 Mar 28;14(4):731. [Abstract]
- Mol Ther Nucleic Acids. 2024 Sep 5;35(4):102322. [Abstract]
- Pharmaceuticals (Basel). 2023 May 3;16(5):692. [Abstract]
- Pharmaceuticals (Basel). 2022 Sep 19;15(9):1161. [Abstract]
- Biomolecules. 2021 Feb 10;11(2):263. [Abstract]
- Sci Rep. 2024 May 11.
- Mol Pharm. 2022 Sep 5;19(9):3217-3227. [Abstract]
- Nucl Med Biol. 2025 May 11:146-147:109028. [Abstract]
- Cancer Biother Radiopharm. 2025 Apr;40(3):219-227. [Abstract]
- J Labelled Comp Radiopharm. 2024 Mar;67(3):111-115. [Abstract]
- Seoul National University. 2025 Jan.
- Res Sq. 2025 Feb 19.
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Drug-Linker Conjugates for ADC アイソフォーム固有の製品をすべて表示
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生物活性
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Traditional Cytotoxic Agents |
Vipivotide tetraxetan (PSMA-617) demonstrates high radiolytic stability for at least 72 h. A high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined) and highly efficient internalization into LNCaP cells are demonstrated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 |
化学情報
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CAS 番号 1702967-37-0
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性状 Solid
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分子量 1042.14
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分子式 C49H71N9O16
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Color White to off-white
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SMILES
O=C(O)[C@H](CCCCNC([C@H](CC1=CC=C2C=CC=CC2=C1)NC([C@H]3CC[C@H](CNC(CN4CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC4)=O)CC3)=O)=O)NC(N[C@H](C(O)=O)CCC(O)=O)=O
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別名
PSMA-617
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (17)
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Journal Impact Factor
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Most Recent
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Biosens Bioelectron
Low cost, high temporal resolution optical fiber-based γ-photon sensor for real-time pre-clinical evaluation of cancer-targeting radiopharmaceuticals. [Abstract]2024 Mar 1:247:115956. PMID: 38145595
Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Biosens Bioelectron. 2024 Mar 1:247:115956. [Abstract]
SPECT scans show progression of 177Lu-Vipivotide tetraxetan (PSMA-617) (i.v.) activity accumulation in PC3-PIP and PC3-flu tumors at five time points taken at the end of every custom γ-probe recording.
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J Nucl Med
Preclinical Evaluation of 177Lu-rhPSMA-10.1, a Radiopharmaceutical for Prostate Cancer: Biodistribution and Therapeutic Efficacy. [Abstract]2025 Apr 1;66(4):599-604. PMID: 40049746
Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: J Nucl Med. 2025 Apr 1;66(4):599-604. [Abstract]
177Lu-Vipivotide tetraxetan (PSMA-617) (30 MBq) significantly suppressed tumor growth from day 18 to day 35 and was well tolerated in the LNCaP xenograft-bearing mice, and no significant weight loss was noted.
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Eur J Nucl Med Mol Imaging
Preliminary evaluation of a novel PSMA-targeting radiopharmaceutical [68Ga]Ga/[177Lu]Lu-NYM032 for theranostic use in prostate cancer. [Abstract]2025 Apr;52(5):1671-1684. PMID: 39745526
Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Eur J Nucl Med Mol Imaging. 2025 Apr;52(5):1671-1684. [Abstract]
Representative torso MIP, CT, and PET/CT imaging with [68Ga]Ga-NYM032 and [68Ga]Ga-Vipivotide tetraxetan (PSMA617) (111 MBq/patient) were performed on the same PCa patients. [68Ga]Ga-Vipivotide tetraxetan (PSMA617) showed good diagnostic efficiency for primary, recurrent, and metastatic PCa lesions.
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Eur J Nucl Med Mol Imaging
2023 Jul;50(8):2342-2352. PMID: 36877233
Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Eur J Nucl Med Mol Imaging. 2023 Jul;50(8):2342-2352. [Abstract]
Representative SPECT images and biodistribution of HepG2 tumor-bearing mice injected with [177Lu]Lu-Vipivotide tetraxetan (PSMA-617) (37 MBq). Tumor uptake of [177Lu]Lu- Vipivotide tetraxetan (PSMA-617) decreased over time indicating rapid blood clearance and short tumor retention time.
Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Eur J Nucl Med Mol Imaging. 2023 Jul;50(8):2342-2352. [Abstract]
Efficacy of radioligand therapy of HepG2 tumor-bearing mice models injected with a single dose of [177Lu]Lu-Vipivotide tetraxetan (PSMA-617) (37 MBq) and [177Lu]Lu-EB-Vipivotide tetraxetan (PSMA-617). Treatment groups exhibited significantly reduced tumor volume and weight compared with the saline group.
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Int J Radiat Oncol Biol Phys
SENTRI: Single-particle Energy Transducer for Radionuclide Injections for Personalized Targeted Radionuclide Cancer Therapy. [Abstract]2024 Apr 1;118(5):1575-1584. PMID: 38122990 -
Pharmaceutics
2022 Mar 28;14(4):731. PMID: 35456565 -
Mol Ther Nucleic Acids
Highly efficient nucleic acid encapsulation method for targeted gene therapy using antibody conjugation system. [Abstract]2024 Sep 5;35(4):102322. PMID: 39363882 -
Pharmaceuticals (Basel)
Characterization of Non-Specific Uptake and Retention Mechanisms of [177Lu]Lu-PSMA-617 in the Salivary Glands. [Abstract]2023 May 3;16(5):692. PMID: 37242475 -
Pharmaceuticals (Basel)
Albumin-Mediated Size Exclusion Chromatography: The Apparent Molecular Weight of PSMA Radioligands as Novel Parameter to Estimate Their Blood Clearance Kinetics. [Abstract]2022 Sep 19;15(9):1161. PMID: 36145382 -
Biomolecules
177Lu-PSMA-617 Therapy in Mice, with or without the Antioxidant α1-Microglobulin (A1M), Including Kidney Damage Assessment Using 99mTc-MAG3 Imaging. [Abstract]2021 Feb 10;11(2):263. PMID: 33579037 -
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Mol Pharm
Evaluation of a Radio-IMmunoStimulant (RIMS) in a Syngeneic Model of Murine Prostate Cancer and ImmunoPET Analysis of T-cell Distribution. [Abstract]2022 Sep 5;19(9):3217-3227. PMID: 35895995 -
Nucl Med Biol
Enhancing the therapeutic index of [211At]YF2 with iodo pseudo carrier: A simple strategy for reducing accumulation in kidneys, salivary and lacrimal glands. [Abstract]2025 May 11:146-147:109028. PMID: 40393125 -
Cancer Biother Radiopharm
Intratumoral Distribution of [177Lu]Lu-PSMA-617 Over Time and in Relation to Diagnostic Tracers in Animal Models of Prostate Cancer. [Abstract]2025 Apr;40(3):219-227. PMID: 39605131 -
J Labelled Comp Radiopharm
Automated radiolabeling and handling of 177 Lu- and 225 Ac-PSMA-617 using a robotic pipettor. [Abstract]2024 Mar;67(3):111-115. PMID: 38296817 -
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溶剤 & 溶解度
DMSO : 100 mg/mL (95.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 100 mg/mL (95.96 mM)
* "≥" means soluble, but saturation unknown.
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.
* 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. 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (2.00 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 (2.00 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (273 KB)
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SDS (393 KB)
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- Deutsch - DE (393 KB)
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取扱説明書 (2659 KB)
参考文献
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 / H2O | 1 mM | 0.9596 mL | 4.7978 mL | 9.5956 mL | 23.9891 mL |
| 5 mM | 0.1919 mL | 0.9596 mL | 1.9191 mL | 4.7978 mL | |
| 10 mM | 0.0960 mL | 0.4798 mL | 0.9596 mL | 2.3989 mL | |
| 15 mM | 0.0640 mL | 0.3199 mL | 0.6397 mL | 1.5993 mL | |
| 20 mM | 0.0480 mL | 0.2399 mL | 0.4798 mL | 1.1995 mL | |
| 25 mM | 0.0384 mL | 0.1919 mL | 0.3838 mL | 0.9596 mL | |
| 30 mM | 0.0320 mL | 0.1599 mL | 0.3199 mL | 0.7996 mL | |
| 40 mM | 0.0240 mL | 0.1199 mL | 0.2399 mL | 0.5997 mL | |
| 50 mM | 0.0192 mL | 0.0960 mL | 0.1919 mL | 0.4798 mL | |
| 60 mM | 0.0160 mL | 0.0800 mL | 0.1599 mL | 0.3998 mL | |
| 80 mM | 0.0120 mL | 0.0600 mL | 0.1199 mL | 0.2999 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.
Vipivotide tetraxetan 関連分類
HY-117410 関連分類
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