HYNIC-iPSMA TFA
Based on 1 Customer Validation
HYNIC-iPSMA TFA is a PSMA-targeted ligand for tumor molecular imaging, with a Ki value of 3.11 nM. HYNIC-iPSMA TFA consists of two components: HYNIC (6-hydrazinonicotinamide) and iPSMA (Inhibitor of Prostate-Specific Membrane Antigen). HYNIC serves as a chelating moiety to link radionuclides to the targeting molecule; iPSMA is a specific inhibitor that targets Prostate-Specific Membrane Antigen (PSMA). 68Ga-labeled iPSMA is used for prostate cancer detection via PET imaging, while the further developed 99mTc-EDDA/HYNIC-iPSMA TFA exhibits excellent specificity and sensitivity. HYNIC-iPSMA TFA can be used for the synthesis and research of radionuclide-conjugated drugs (RDC).
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- Pureté : 98.05%
- CAS No.: 2375849-11-7
- Formule: C33H38F3N7O11
- Masse moléculaire:765.69
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Stockage:
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)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
HYNIC-iPSMA (5 mg in 98 mL solution; 24 h) TFA can be formulated into a sterile, pyrogen-free lyophilized kit, which maintains stability for 1 year and enables efficient radiolabeling with 99mTc[1].
HYNIC-iPSMA (1 h) TFA potently binds to PSMA on LNCaP cells, with a Ki value of 3.11 nM[3].
HYNIC-iPSMA (10 mg; 15 min) TFA enables efficient synthesis of [99mTc]Tc-HYNIC-iPSMA TFA with radiochemical purity ≥95%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
99mTc-EDDA/HYNIC-iPSMA (3.7 MBq; i.v.; single dose) TFA shows negligible uptake in PSMA-negative PC-3 tumors in nude mice, confirming PSMA-specific targeting[1].
99mTc]Tc-EDDA/HYNIC-iPSMA (~2-20 MBq; i.v.; single dose) TFA achieves a tumor uptake of 10.3 %ID/g at 1 h post-injection in LNCaP tumor-bearing NRG mice, with high off-target uptake in kidneys, spleen, and salivary glands[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude (male, 6-7 weeks old, 20-22 g, subcutaneous injection of 1×106 LNCaP PSMA-positive human prostate cancer cells)[1]
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Dosage:3.7 MBq
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Administration:i.v.; single dose
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Result:Achieved tumor uptake of 10.22% ID/g at 1 h and 9.84% ID/g at 3 h in unblocked mice.
Reached tumor-to-blood ratios of 62.33 at 1 h and 271 at 3 h in unblocked mice.
Reduced tumor uptake to 2.93% ID/g at 3 h in blocked mice, with a tumor-to-blood ratio of 12.74.
Showed a tumor standardized uptake value (SUV) of 7.3 in unblocked mice, which decreased to 3.2 in blocked mice.
Exhibited high kidney uptake of 23.63% ID/g at 1 h and 12.63% ID/g at 3 h.
Demonstrated moderate liver uptake of 2.18% ID/g at 1 h and 1.42% ID/g at 3 h.
Achieved rapid blood clearance of 0.18% ID/g at 1 h and 0.04% ID/g at 3 h.
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Animal Model:Athymic nude (male, 6-7 weeks old, 20-22 g, subcutaneous injection of 1×106 PC-3 PSMA-negative human prostate cancer cells)[1]
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Dosage:3.7 MBq
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Administration:i.v.; single dose
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Result:Showed negligible tumor uptake of 0.23% ID/g at 1 h and 0.06% ID/g at 3 h.
Reached tumor-to-blood ratios of 1.05 at 1 h and 1.20 at 3 h.
Exhibited high kidney uptake of 25.11% ID/g at 1 h and 13.14% ID/g at 3 h.
Demonstrated moderate liver uptake of 2.21% ID/g at 1 h and 1.57% ID/g at 3 h.
Achieved rapid blood clearance of 0.22% ID/g at 1 h and 0.05% ID/g at 3 h.
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Animal Model:NOD-Rag1nullIL2rgnull (NRG) (male, subcutaneous inoculation with LNCaP cells, studied 5-6 weeks post-inoculation)[3]
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Dosage:~20 MBq (imaging); ~2 MBq (biodistribution)
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Administration:i.v.; single dose
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Result:Achieved a tumor uptake of 10.3 %ID/g, kidney uptake of 45.3 %ID/g, spleen uptake of 23.4 %ID/g, salivary gland uptake of 7.77 %ID/g, and minimal liver uptake of 0.45 %ID/g at 1 h post-injection.
Reached tumor-to-background ratios of 22.3 (tumor-to-bone), 21.8 (tumor-to-muscle), 15.4 (tumor-to-blood), and 0.33 (tumor-to-kidney) at 1 h post-injection.
Was excreted mainly via the renal pathway.
Successfully visualized LNCaP tumor xenografts in SPECT images.
Chemical Information
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CAS No. 2375849-11-7
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Appearance Solid
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Masse moléculaire 765.69
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Formule C33H38F3N7O11
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Color White to off-white
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Sequence
Hydrazinonicotinyl-Lys(Nal)-Urea-Glu
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Sequence Shortening
Hydrazinonicotinyl-Lys(Nal)-Urea-Glu
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (130.60 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 (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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (278 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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Instruction de manipulation (2659 KB)
Références
[1]. Ferro-Flores G, et al. Clinical translation of a PSMA inhibitor for 99mTc-based SPECT. Nucl Med Biol. 2017 May;48:36-44. [Content Brief]
[2]. Tually P, et al. Real world experience with [Tc]Tc-HYNIC-iPSMA SPECT prostate cancer detection: interim results from the global NOBLE registry. EJNMMI reports. 2024 Dec 30;8(1):43. [Content Brief]
[3]. Lu K, et al. Synthesis and Evaluation of 99mTc-Labeled PSMA-Targeted Tracers Based on the Lys-Urea-Aad Pharmacophore for Detecting Prostate Cancer with Single Photon Emission Computed Tomography. Molecules. 2023 Jun 29;28(13):5120. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3060 mL | 6.5301 mL | 13.0601 mL | 32.6503 mL |
| 5 mM | 0.2612 mL | 1.3060 mL | 2.6120 mL | 6.5301 mL | |
| 10 mM | 0.1306 mL | 0.6530 mL | 1.3060 mL | 3.2650 mL | |
| 15 mM | 0.0871 mL | 0.4353 mL | 0.8707 mL | 2.1767 mL | |
| 20 mM | 0.0653 mL | 0.3265 mL | 0.6530 mL | 1.6325 mL | |
| 25 mM | 0.0522 mL | 0.2612 mL | 0.5224 mL | 1.3060 mL | |
| 30 mM | 0.0435 mL | 0.2177 mL | 0.4353 mL | 1.0883 mL | |
| 40 mM | 0.0327 mL | 0.1633 mL | 0.3265 mL | 0.8163 mL | |
| 50 mM | 0.0261 mL | 0.1306 mL | 0.2612 mL | 0.6530 mL | |
| 60 mM | 0.0218 mL | 0.1088 mL | 0.2177 mL | 0.5442 mL | |
| 80 mM | 0.0163 mL | 0.0816 mL | 0.1633 mL | 0.4081 mL | |
| 100 mM | 0.0131 mL | 0.0653 mL | 0.1306 mL | 0.3265 mL |
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