NOTA-cRY9M
NOTA-cRY9M is a reagent targeting FGFR1 with a Kd value of 58 nM, and exhibits subtype selectivity for FGFR2-4. When radiolabeled as [68Ga]Ga-NOTA-cRY9M, it functions as a stabilizer, imaging contrast enhancer, and tumor-targeting agent, and accumulates in FGFR1-positive non-small cell lung cancer xenograft models. NOTA-cRY9M can be used in studies related to non-small cell lung cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C71H108N26O17
- Masse moléculaire:1597.78
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
FGFR1 58 nM (Kd) |
68Ga]Ga-NOTA-cRY9M (74 kBq per well; 15-120 min) exhibits time-dependent, FGFR1-specific cellular uptake in Calu-3 and NCI-H520 NSCLC cells, with significantly lower uptake in FGFR1-negative NCI-H2170 cells[1].
[68Ga]Ga-NOTA-cRY9M (74 kBq per well; 10-11-10-2 M unlabeled peptide; 2 h) exhibits high FGFR1-binding affinity in Calu-3 cells, with an IC50 of 62 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude (male, 4-5 weeks old, 18-21 g)[1]
-
Dosage:3.7 MBq
-
Administration:i.v.; single dose
-
Result:Achieved peak tumor uptake of 3.69 %ID/g at 10 minutes postinjection, with uptake declining gradually to 3.33 %ID/g by 60 minutes.
Reached a maximum tumor-to-muscle ratio of 5.56 at 60 minutes, with tumor-to-liver and tumor-to-lung ratios reaching approximately 2.3 and 3.3, respectively, at 60 minutes.
Exhibited primarily renal excretion with low hepatic retention.\nAchieved peak tumor uptake of 3.11 %ID/g at 10 minutes postinjection.
Reached a maximum tumor-to-muscle ratio of 4.10 at 60 minutes.
Showed tumor uptake of 2.61 %ID/g in ex vivo biodistribution at 60 minutes.\nAchieved a maximum tumor uptake of 1.20 %ID/g, with a consistently low tumor-to-muscle ratio of 1.42 throughout the 60-minute imaging window.
Showed tumor uptake of 0.91 %ID/g in ex vivo biodistribution at 60 minutes.\nShowed a substantial reduction in [68Ga]Ga-NOTA-cRY9M uptake (1.10 %ID/g) in FGFR1-knockdown Calu-3 xenografts compared to control Calu-3 tumors (3.83 %ID/g), with a corresponding tumor-to-muscle ratio of 2.11 vs. 5.89 in controls.
Chemical Information
-
Masse moléculaire 1597.78
-
Formule C71H108N26O17
-
Sequence
Cyclo(Arg-Trp-Arg-{Lys(NOTA)}-Gln-Thr-Arg-His-Tyr)
-
Sequence Shortening
Cyclo(RWR-{Lys(NOTA)}-QTRHY)
-
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
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)