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.
For research use only. We do not sell to patients.
- Formula: C80H119N19O21
- Molecular Weight:1682.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Radionuclide-Drug Conjugates (RDCs) Isoforms
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Biological Activity
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RDC Peptide |
[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 Kd value of 0.12 nM[1].
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 Kd 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.
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Cell Line:human prostate adenocarcinoma PC3 cells
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Concentration:1.85 MBq lutetium-177-labelled LF1
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Incubation Time:72 h
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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.
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.
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Animal Model:Balb/C nude (male, 6 weeks old, 20-25 g, subcutaneously implanted with PC-3 cells)[1]
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Dosage:41.2 MBq (1200 pmol total, 6 fractional doses); 93.4 MBq (2400 pmol total, 6 fractional doses)
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Administration:6 fractional doses over two 3-day periods separated by a 1-week interval
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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
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Molecular Weight 1682.92
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Formula C80H119N19O21
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Sequence
{AAZTA-Pip-d-Phe}-Gln-Trp-Ala-Val-Gly-His-{Sta}-Leu-NH2
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Sequence Shortening
{AAZTA-Pip-d-Phe}-QWAVGH-{Sta}-L-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LF1 Related Classifications
HY-P11917 Related Classifications
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