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Cat. No.: HY-P11917

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LF1

LF1 is a gastrin-releasing peptide receptor (GRPR) antagonist. LF1 can be stably radiolabeled with gallium-⁶⁸, indium-¹¹¹, and lutetium-¹⁷⁷. Radiolabeled LF1 can be used for high-contrast SPECT/CT imaging. LF1 is applicable to prostate cancer-related research.

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Formule: C₈₀H₁₁₉N₁₉O₂₁
Masse moléculaire:1682.92

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Synthèse personnalisée de peptides

LF1 Chemical Structure

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Use of MCE Products

One-Stop Platform：From Independent R&D to Pilot-Scale Production

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

RDC Peptide

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In Vitro

OthersAnti-cancer

Others

[¹⁷⁷Lu]Lu-LF1 (1-3 nM) binds to GRPR-expressing prostate cancer PC-3 cells with high affinity and desirable slow dissociation kinetics, with a K_d value of 0.12 nM^[1].

Anti-cancer

⁶⁸/natGa-LF1, ¹⁷⁷/natLu-LF1, and ¹¹¹/natIn-LF1 (1-100 nM; 120 min) bind to GRPr on PC3 cells with high affinity, with K_d values of 16.3 nM, 10.2 nM, and 5.2 nM, respectively^[2].
The combination strategy of Rapamycin (HY-10219) and Lutetium-¹⁷⁷-labelled LF1 (72 h) reduces the viability of PC3 cells more effectively than either agent used alone, with cell viability decreasing to approximately 40% at 72 h^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:

human prostate adenocarcinoma PC3 cells
Concentration:

1.85 MBq lutetium-177-labelled LF1
Incubation Time:

72 h
Result:

Resulted in ~70% cell viability at 72 h for lutetium-177-labelled LF1 monotherapy.
Resulted in ~50% cell viability at 72 h for rapamycin monotherapy.
Resulted in ~40% cell viability at 72 h for combination therapy with rapamycin and lutetium-177-labelled LF1.

In Vivo

Anti-cancer

[¹⁷⁷Lu]Lu-LF1 (41.2-93.4 MBq; administered in 6 fractions over two 3-day cycles with a 1-week interval between cycles) exhibits a dose-dependent effect in PC-3 tumor-bearing mice, where the fractionated dose of 93.4 MBq induces significant tumor inhibition with a median survival time of 50 days^[1].
Combination therapy with a single dose of [¹⁷⁷Lu]Lu-LF1 (40 MBq) and pretreatment with Everolimus (HY-10218) enhances tumor control in PC-3 tumor-bearing mice and prolongs their median survival to 38 days, whereas a single dose of [¹⁷⁷Lu]Lu-LF1 alone yields no significant benefit^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Balb/C nude (male, 6 weeks old, 20-25 g, subcutaneously implanted with PC-3 cells)^[1]
Dosage:

41.2 MBq (1200 pmol total, 6 fractional doses); 93.4 MBq (2400 pmol total, 6 fractional doses)
Administration:

6 fractional doses over two 3-day periods separated by a 1-week interval
Result:

Showed limited tumor control and reached study end points within 25 days, with a median survival of 16 days (41.2 MBq dose).
Exhibited significant tumor suppression, with tumor volumes remaining under 400 mm³ for at least the first 25 days, and had a median survival of 50 days, with two mice surviving past 104 and 127 days (93.4 MBq dose).
Remained stable across all treated groups (body weight).

Chemical Information

Masse moléculaire 1682.92
Formule C₈₀H₁₁₉N₁₉O₂₁
Sequence

{AAZTA-Pip-d-Phe}-Gln-Trp-Ala-Val-Gly-His-{Sta}-Leu-NH2
Sequence Shortening

{AAZTA-Pip-d-Phe}-QWAVGH-{Sta}-L-NH2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Kumar N, et al. Preclinical Evaluation of a Lu-Labeled Gastrin-Releasing Peptide Receptor Antagonist and Prostate Cancer Treatment with Monotherapy and in Combination with Everolimus. ACS pharmacology & translational science. 2026 Jan 09;9(1):59-68.

[2]. Hofstetter M, et al. Effect of the versatile bifunctional chelator AAZTA on the radiometal labelling properties and the in vitro performance of a gastrin releasing peptide receptor antagonist. EJNMMI radiopharmacy and chemistry. 2020 Nov 30;5(1):29.

Calculators

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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LF1

Voir tous les produits spécifiques à Isoform Radionuclide-Drug Conjugates (RDCs)