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Art. -Nr.: HY-P12120

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ErbB-2-binding peptide-2

(Synonyms: KCCYSL)

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. Nr.: 499773-67-0
Formel: C₃₀H₄₉N₇O₉S₂
Molecular Weight:715.88

Speicherung:

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

ErbB-2-binding peptide-2 Chemical Structure

CAS. Nr.: 499773-67-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
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Calculators
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Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HER2

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In Vitro

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.

In Vivo

¹¹¹In-DOTA-GSG-KCCYSL (0.185-11.1 MBq; intravenous bolus; single administration) exhibits specific, time-dependent tumor uptake in ovcar-3 xenografted scid mice, with clear tumor visualization via SPECT/CT at 2 h post-injection; tumor uptake decreases by 59% when blocked by non-radioactively labeled peptides^[1].
^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.

Animal Model:

scid (ICR scid) (female, 4-6 week old)^[1]
Dosage:

0.185 MBq (5 μCi) (tissue uptake); 11.1 MBq (300 μCi) (imaging); 100 μg (blocking)
Administration:

i.v. bolus; single dose
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.

Animal Model:

SCID mice^[2]
Dosage:

76 nmol/mouse
Administration:

single injection 10 minutes prior to radiolabeled conjugate
Result:

Reduced tumor radioactivity (from co-administered radiolabeled conjugate) by 50% at 2 hours post-injection.
Showed minimal inhibition in normal tissues.

Chemical Information

CAS. Nr. 499773-67-0
Molecular Weight 715.88
Formel C₃₀H₄₉N₇O₉S₂
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
Synonyms

KCCYSL
Sequence

Lys-Cys-Cys-Tyr-Ser-Leu
Sequence Shortening

KCCYSL
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Deutscher SL, et al. In-labeled KCCYSL peptide as an imaging probe for ErbB-2-expressing ovarian carcinomas. Journal of labelled compounds & radiopharmaceuticals. 2009 Dec 01;52(14):583-590. [Content Brief]

[2]. Leung, K. (2012). 64Cu-Bis (carboxymethyl)-1, 4, 8, 11-tetraazabicyclo [6.6. 2] hexadecane-(Gly-Ser-Gly)-Lys-Cys-Cys-Tyr-Ser-Leu. Molecular Imaging and Contrast Agent Database (MICAD)[Internet].

Calculators

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)}

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.

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Biologische Aktivität
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- IC₅₀ & Target
- In Vitro
- In Vivo
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ErbB-2-binding peptide-2

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Biologische Aktivität

Chemical Information

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Verweise

Calculators

Help & FAQs

ErbB-2-binding peptide-2 Related Classifications

HY-P12120 Related Classifications