HYNIC-iPSMA
HYNIC-iPSMA is a PSMA-targeted ligand for tumor molecular imaging, with a Ki value of 3.11 nM. HYNIC-iPSMA consists of two components: HYNIC (6-hydrazinonicotinamide) and iPSMA (Inhibitor of Prostate-Specific Membrane Antigen). HYNIC acts 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 can be used for the synthesis and research of radionuclide-conjugated drugs (RDC).
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- CAS No.: 2192215-74-8
- 화학식: C31H37N7O9
- 분자량:651.67
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Radionuclide-Drug Conjugates (RDCs) Isoforms
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Biological Activity
HYNIC-iPSMA (5 mg in 98 mL solution; 24 h) 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) potently binds to PSMA on LNCaP cells, with a Ki value of 3.11 nM[3].
HYNIC-iPSMA (10 mg; 15 min) enables efficient synthesis of [99mTc]Tc-HYNIC-iPSMA with radiochemical purity ≥95%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
99mTc-EDDA/HYNIC-iPSMA (3.7 MBq; i.v.; single dose) 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) 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. 2192215-74-8
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분자량 651.67
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화학식 C31H37N7O9
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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