PNT2001
Based on 1 Customer Validation
PNT2001 (LY4181530) is a high-affinity PSMA-targeted radiopharmaceutical ligand precursor. natLu-PNT2001 has an IC50 of 3.1 nM against PSMA. PNT2001 is applicable for PSMA targeting, radiopharmaceutical ligand delivery, and prostate cancer-related research.
For research use only. We do not sell to patients.
- Purity: 98.72%
- CAS No.: 2790413-59-9
- Formula: C85H107N15O32
- Molecular Weight:1850.84
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Storage:
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PSMA 3.1 nM (IC50, natLu-PNT2001) |
PNT2001 (natLu-PNT2001) (LY4181530) binds to PSMA in PSMA-positive LNCaP cell competitive binding assays, with an IC50 of 3.1 nM[2].
The internalization level of PNT2001 (177Lu-PNT2001) in PSMA-positive LNCaP cells is approximately 3.4-fold that of 177Lu-PSMA-I&T[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PNT2001 (177Lu-PSMA-62; approximately 5-6 MBq, 160 pmol; intravenous injection; single dose) exhibits PSMA-dependent tumor targeting in LNCaP tumor-bearing CB17-SCID mice. Co-administration of the PSMA inhibitor 2-PMPA (HY-100788) (6.4 nmol) significantly reduces tumor uptake at 24 h post-administration[1].
PNT2001 (225Ac-PNT2001; 10-40 kBq; intravenous injection; single administration) dose-dependently inhibits tumor growth and prolongs survival in NSG mice bearing ~200 mm3 subcutaneous LNCaP xenografts[1].
PNT2001 (225Ac-PNT2001; 20 or 40 kBq; intravenous injection; single administration) inhibits the growth of large subcutaneous LNCaP tumors in NSG mice, with 40 kBq inducing sustained tumor control and enabling multiple mice to survive for over 100 days[1].
PNT2001 (225Ac-PNT2001; 40 kBq; intravenous injection; single administration) significantly reduces tumor burden and prolongs survival in NSG mice bearing PSMA-positive C4-2 metastatic tumors expressing luciferase, and exhibits stronger antitumor activity than 225Ac-PSMA-I&T at the same radioactivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17-SCID (male/female not specified; bearing subcutaneous LNCaP tumors, 150-500 mm3)[1]
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Dosage:5-6 MBq; 160 pmol
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Administration:i.v.; single dose
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Result:Exhibited kidney uptake of 14.45 %ID/g, tumor retention of 13.03 %ID/g, and a tumor:kidney ratio of 0.902 at 24 hours post-injection.
Reduced tumor uptake to 3.5-4.9 %ID/g and kidney uptake to 2.6-2.9 %ID/g when co-injected with 2-PMPA, confirming target-specific binding.
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Animal Model:NSG (male/female not specified; bearing subcutaneous LNCaP tumors, ~200 mm3)[1]
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Dosage:10 kBq; 20 kBq; 40 kBq
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Administration:i.v.; single dose
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Result:Slowed tumor growth compared to vehicle, with significantly reduced tumor volumes in the 10 kBq, 20 kBq, and 40 kBq groups on day 35.
Achieved durable tumor control and long-term survival >100 days in multiple mice in the 40 kBq group.
Was well tolerated by all mice, with minimal body weight loss.
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Animal Model:NSG (male/female not specified; bearing subcutaneous LNCaP tumors, ~800 mm3)[1]
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Dosage:20 kBq; 40 kBq
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Administration:i.v.; single dose
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Result:Slowed large tumor growth compared to vehicle and precursor controls, with significantly reduced tumor volumes in the 40 kBq group on day 21, and reduced tumor volume in the 20 kBq group relative to vehicle.
Improved survival in the 40 kBq group.
Was well tolerated by all mice, with minimal body weight loss.
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Animal Model:NSG (male/female not specified; injected via tail vein with luciferase-enabled PSMA+ C4-2 tumor cells)[1]
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Dosage:40 kBq
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Administration:i.v.; single dose
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Result:Significantly controlled metastatic lesion formation, with drastically reduced BLI signal compared to vehicle and 225Ac-PSMA-I&T groups, reaching near baseline on day 29.
Significantly improved survival compared to vehicle and 225Ac-PSMA-I&T, with 100% survival up to day 120.
Was well tolerated by mice, with stable body weight.
Chemical Information
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CAS No. 2790413-59-9
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Appearance Solid
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Molecular Weight 1850.84
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Formula C85H107N15O32
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Color White to off-white
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Synonyms
LY4181530; PSMA-62
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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)
Solvent & Solubility
DMSO : ≥ 50 mg/mL (27.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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 (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)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
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 | 0.5403 mL | 2.7015 mL | 5.4030 mL | 13.5074 mL |
| 5 mM | 0.1081 mL | 0.5403 mL | 1.0806 mL | 2.7015 mL | |
| 10 mM | 0.0540 mL | 0.2701 mL | 0.5403 mL | 1.3507 mL | |
| 15 mM | 0.0360 mL | 0.1801 mL | 0.3602 mL | 0.9005 mL | |
| 20 mM | 0.0270 mL | 0.1351 mL | 0.2701 mL | 0.6754 mL | |
| 25 mM | 0.0216 mL | 0.1081 mL | 0.2161 mL | 0.5403 mL |
PNT2001 Related Classifications
HY-P6825 Related Classifications
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- PNT2001
- 2790413-59-9
- LY4181530
- PSMA-62
- PNT 2001
- PNT-2001
- LY 4181530
- LY-4181530
- PSMA62
- PSMA 62
- PSMA-62
- PSMA
- prostate cancer cells
- LNCaP prostate cancer cells
- CB17-SCID mice
- oligometastatic hormone-sensitive prostate cancer
- metastatic prostate cancer
- NSG mice
- metastatic castration-resistant prostate cancer
- prostate cancer
- Inhibitor
- inhibitor
- inhibit