Art. -Nr.: HY-P5292A

HYNIC-iPSMA TFA

Name: HYNIC-iPSMA TFA
Brand: MedChemExpress
SKU: HY-P5292A
Price: 310.00 USD
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HYNIC-iPSMA TFA is a PSMA-targeted ligand for tumor molecular imaging, with a K_i 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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Reinheit : 98.05%
CAS. Nr.: 2375849-11-7
Formel: C₃₃H₃₈F₃N₇O₁₁
Molecular Weight:765.69

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)

HYNIC-iPSMA TFA Chemical Structure

CAS. Nr.: 2375849-11-7

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Radionuclide-Drug Conjugates (RDCs) Isoform-spezifische Produkte anzeigen :

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 K_i 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 demonstrates specific, high PSMA-mediated tumor uptake in LNCaP tumor-bearing nude mice, reaching 9.84% ID/g at 3 h post-injection, with rapid blood clearance and primarily renal elimination^[1].
^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.

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]
Dosage:

3.7 MBq
Administration:

i.v.; single dose
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.

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]
Dosage:

3.7 MBq
Administration:

i.v.; single dose
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.

Animal Model:

NOD-Rag1nullIL2rgnull (NRG) (male, subcutaneous inoculation with LNCaP cells, studied 5-6 weeks post-inoculation)^[3]
Dosage:

~20 MBq (imaging); ~2 MBq (biodistribution)
Administration:

i.v.; single dose
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

CAS. Nr. 2375849-11-7
Appearance Solid
Molecular Weight 765.69
Formel C₃₃H₃₈F₃N₇O₁₁
Color White to off-white
Sequence

Hydrazinonicotinyl-Lys(Nal)-Urea-Glu
Sequence Shortening

Hydrazinonicotinyl-Lys(Nal)-Urea-Glu
Versand

Room temperature in continental US; may vary elsewhere.

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)

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.3060 mL

6.5301 mL

13.0601 mL

5 mM

0.2612 mL

1.3060 mL

2.6120 mL

10 mM

0.1306 mL

0.6530 mL

1.3060 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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HYNIC-iPSMA TFA

Alle Radionuclide-Drug Conjugates (RDCs) Isoform-spezifische Produkte anzeigen