Zadavotide guraxetan
Based on 3 publication(s) in Google Scholar
Zadavotide guraxetan (PSMA I&T; PNT-2002) is an effective inhibitor of prostate-specific membrane antigen (PSMA). Zadavotide guraxetan can be used for SPECT/CT imaging and radionuclide studies in triple-negative breast cancer and prostate cancer (PCa).
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- Pureté : 99.87%
- CAS No.: 2192281-54-0
- Formule: C63H92IN11O23
- Masse moléculaire:1498.37
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Zadavotide guraxetan
More
Activité biologique
Description
IC50 & Target
PSMA[1]
In Vitro
Zadavotide guraxetan has high specificity for PSMA-expressing PCa cells, xenografted PCa, and in vitro kidneys, with equilibrium binding constants Kd of 3.9 nM and 5.6 nM for LNCaP and LS174T-PSMA, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice injected with LNCaP or LS174T-PSMA cells[1]
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Dosage:0.1-1 nM (0.2 MBq); single dose
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Administration:Intravenous injection (i.v.)
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Result:Showed dose-dependent uptake in PSMA-expressing tumors, kidney, spleen, adrenal glands, lung, and salivary glands.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2192281-54-0
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Appearance Solid
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Masse moléculaire 1498.37
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Formule C63H92IN11O23
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Color White to off-white
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SMILES
IC(C=C1C[C@H](C(N[C@@H](C(N[C@@H](C(O)=O)CCCCNC(CCCCCCC(NCCCC[C@@H](C(O)=O)NC(N[C@H](C(O)=O)CCC(O)=O)=O)=O)=O)=O)CC2=CC=CC=C2)=O)NC(CCC(N3CCN(CCN(CCN(CC3)CC(O)=O)CC(O)=O)CC(O)=O)C(O)=O)=O)=C(C=C1)O
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Synonyms
PSMA I&T; PNT-2002
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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)
Publications (3)
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Journal Impact Factor
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Most Recent
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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 -
Mol Imaging Biol
2025 Sep 2. PMID: 40897948
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (66.74 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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)
In Vivo:
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: ≥ 1.25 mg/mL (0.83 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (0.83 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Chatalic KL, et al. Towards Personalized Treatment of Prostate Cancer: PSMA I&T, a Promising Prostate-Specific Membrane Antigen-Targeted Theranostic Agent. Theranostics. 2016 Apr 12;6(6):849-61. [Content Brief]
[2]. Amelie Heesch, et al. The prostate-specific membrane antigen holds potential as a vascular target for endogenous radiotherapy with [177Lu]Lu-PSMA-I&T for triple-negative breast cancer. Breast Cancer Res. 2024 Feb 20;26(1):30. [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 |
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| DMSO | 1 mM | 0.6674 mL | 3.3370 mL | 6.6739 mL | 16.6848 mL |
| 5 mM | 0.1335 mL | 0.6674 mL | 1.3348 mL | 3.3370 mL | |
| 10 mM | 0.0667 mL | 0.3337 mL | 0.6674 mL | 1.6685 mL | |
| 15 mM | 0.0445 mL | 0.2225 mL | 0.4449 mL | 1.1123 mL | |
| 20 mM | 0.0334 mL | 0.1668 mL | 0.3337 mL | 0.8342 mL | |
| 25 mM | 0.0267 mL | 0.1335 mL | 0.2670 mL | 0.6674 mL | |
| 30 mM | 0.0222 mL | 0.1112 mL | 0.2225 mL | 0.5562 mL | |
| 40 mM | 0.0167 mL | 0.0834 mL | 0.1668 mL | 0.4171 mL | |
| 50 mM | 0.0133 mL | 0.0667 mL | 0.1335 mL | 0.3337 mL | |
| 60 mM | 0.0111 mL | 0.0556 mL | 0.1112 mL | 0.2781 mL |
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