Art. -Nr.: HY-P6825

Ancelvotide Guraxetan

Name: Ancelvotide Guraxetan
Brand: MedChemExpress
SKU: HY-P6825
Price: 160.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: PNT2001; LY4181530; PSMA-62)

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Ancelvotide Guraxetan (PNT2001) is a high-affinity PSMA-targeted radiopharmaceutical ligand precursor. natLu-Ancelvotide Guraxetan has an IC₅₀ of 3.1 nM against PSMA. Ancelvotide Guraxetan is applicable for PSMA targeting, radiopharmaceutical ligand delivery, and prostate cancer-related research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 98.72%
CAS. Nr.: 2790413-59-9
Formel: C₈₅H₁₀₇N₁₅O₃₂
Molecular Weight:1850.84

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)

Ancelvotide Guraxetan Chemical Structure

CAS. Nr.: 2790413-59-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

PSMA

3.1 nM (IC₅₀, natLu-PNT2001)

In Vitro

Anti-cancer

Ancelvotide Guraxetan (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 Ancelvotide Guraxetan (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.

In Vivo

Anti-cancer

Ancelvotide Guraxetan (¹⁷⁷Lu-PNT2001; approximately 5-6 MBq, 160 pmol; intravenous injection; single dose) exhibits high tumor retention and low renal uptake in subcutaneous LNCaP tumor-bearing CB17-SCID mice. At 24 h post-administration, the tumor and renal uptake values are 13.03 and 14.45 %ID/g, respectively, with a tumor-to-kidney ratio of 0.902^[1].
Ancelvotide Guraxetan (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].
Ancelvotide Guraxetan (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].
Ancelvotide Guraxetan (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].
Ancelvotide Guraxetan (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.

Animal Model:

CB17-SCID (male/female not specified; bearing subcutaneous LNCaP tumors, 150-500 mm³)^[1]
Dosage:

5-6 MBq; 160 pmol
Administration:

i.v.; single dose
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.

Animal Model:

NSG (male/female not specified; bearing subcutaneous LNCaP tumors, ~200 mm³)^[1]
Dosage:

10 kBq; 20 kBq; 40 kBq
Administration:

i.v.; single dose
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.

Animal Model:

NSG (male/female not specified; bearing subcutaneous LNCaP tumors, ~800 mm³)^[1]
Dosage:

20 kBq; 40 kBq
Administration:

i.v.; single dose
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.

Animal Model:

NSG (male/female not specified; injected via tail vein with luciferase-enabled PSMA+ C4-2 tumor cells)^[1]
Dosage:

40 kBq
Administration:

i.v.; single dose
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

CAS. Nr. 2790413-59-9
Appearance Solid
Molecular Weight 1850.84
Formel C₈₅H₁₀₇N₁₅O₃₂
Color White to off-white
Synonyms

PNT2001; LY4181530; PSMA-62
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 : ≥ 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.

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

0.5403 mL

2.7015 mL

5.4030 mL

5 mM

0.1081 mL

0.5403 mL

1.0806 mL

10 mM

0.0540 mL

0.2701 mL

0.5403 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)}

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 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]. Vito A, et al. Development and characterization of ²²⁵Ac-PNT2001, a next-generation PSMA radioligand. EANM E-Poster. 2022.

[2]. Saleh R, et al. ACCEL: [²²⁵Ac]-PSMA-62 Phase Ia/Ib/II clinical trial to characterize efficacy, safety, tolerability, and dosimetry in oligometastatic hormone-sensitive and metastatic castration-resistant prostate cancer. TPS282 Trials in Progress Poster Session. 2026.

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	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

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Ancelvotide Guraxetan