ErbB-2-binding peptide-2
ErbB-2-binding peptide-2 (KCCYSL) is a peptide targeting ErbB-2/HER2, which specifically binds to the extracellular domain of HER2 and accumulates in HER2-expressing cancer cells. When radiolabeled, ErbB-2-binding peptide-2 serves as a SPECT/CT and PET imaging agent, enabling the visualization of HER2-expressing tumor xenografts. ErbB-2-binding peptide-2 is applicable to research related to ovarian cancer and breast cancer.
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- CAS No.: 499773-67-0
- Formule: C30H49N7O9S2
- Masse moléculaire:715.88
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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HER2 |
111In-DOTA-GSG-KCCYSL (45 min) exhibits nanomolar binding affinity to ErbB-2-expressing human ovarian cancer cell line OVCAR-3, with an IC50 value of 47 nM[1].
111In-DOTA-GSG-KCCYSL (3×104 cpm; 90 min) specifically binds to ErbB-2-expressing OVCAR-3 human ovarian cancer cells, reaching binding equilibrium at 90 min, whereas its binding to HIO-80 normal ovarian epithelial cells with low ErbB-2 expression is extremely low[1].
ErbB-2-binding peptide-2 (45 min) mediates time-dependent, HER2-specific binding to human MDA-MB-435 breast cancer cells, and its non-radiolabeled conjugated analog natCu-CB-TE2A-(GSG)-KCCYSL has a measured IC50 of 31 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
natCu-CB-TE2A-(GSG)-KCCYSL (76 nmol per mouse; single injection administered 10 minutes prior to injection of the radiolabeled conjugate) reduces the tumor uptake of the corresponding radiolabeled conjugate by 50% at 2 hours post-injection in a HER2-positive MDA-MB-435 breast cancer xenograft model in SCID mice[2].
64Cu-CB-TE2A-(GSG)-KCCYSL enables clear PET imaging of HER2-expressing MDA-MB-435 breast cancer xenografts in SCID mice at 2 h post-injection[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:scid (ICR scid) (female, 4-6 week old)[1]
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Dosage:0.185 MBq (5 μCi) (tissue uptake); 11.1 MBq (300 μCi) (imaging); 100 μg (blocking)
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Administration:i.v. bolus; single dose
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Result:Reached tumor uptake of 0.50 %ID/g at 1 hour, 0.39 %ID/g at 2 hours, 0.15 %ID/g at 4 hours, and 0.09 %ID/g at 24 hours post-injection.
Achieved tumor-to-muscle ratio of 13.0 and tumor-to-blood ratio of 3.0 at 2 hours post-injection.
Reduced tumor uptake of the radiolabeled reagent by approximately 59% (P = 0.04) when pre-administered with non-radiolabeled peptide.
Enabled clear visualization of ovcar-3 tumor xenografts via microSPECT/microCT imaging at 2 hours post-injection, with minimal background radioactivity except for substantial uptake in kidneys.
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Animal Model:SCID mice[2]
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Dosage:76 nmol/mouse
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Administration:single injection 10 minutes prior to radiolabeled conjugate
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Result:Reduced tumor radioactivity (from co-administered radiolabeled conjugate) by 50% at 2 hours post-injection.
Showed minimal inhibition in normal tissues.
Chemical Information
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CAS No. 499773-67-0
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Masse moléculaire 715.88
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Formule C30H49N7O9S2
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SMILES
O=C(N[C@@H](CS)C(N[C@@H](CS)C(N[C@@H](CC1=CC=C(C=C1)O)C(N[C@@H](CO)C(N[C@@H](CC(C)C)C(O)=O)=O)=O)=O)=O)[C@H](CCCCN)N
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Synonyms
KCCYSL
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Sequence
Lys-Cys-Cys-Tyr-Ser-Leu
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Sequence Shortening
KCCYSL
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Livraison
Room temperature in continental US; may vary elsewhere.
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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)
ErbB-2-binding peptide-2 Related Classifications
HY-P12120 Related Classifications
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- ErbB-2-binding peptide-2
- 499773-67-0
- KCCYSL
- EGFR
- Radionuclide-Drug Conjugates (RDCs)
- HER2
- HER2-expressing cancer cells
- MDA-MB-435 breast carcinoma cells
- OVCAR-3 human ovarian carcinoma cells
- HIO-80 normal ovarian epithelial cells
- tumor xenografts
- ovarian carcinoma
- ErbB-2
- SCID mice
- breast cancer
- Inhibitor
- inhibitor
- inhibit