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  3. WGYRGFYC

WGYRGFYC (WC8) is a selective HER2-targeting peptide that binds specifically to HER2 by mimicking the antigen-binding site of trastuzumab. The DOTA precursor of WGYRGFYC has a KD of 61.20 nM for HER2. WGYRGFYC enables specific and highly sensitive detection of HER2 expression in HER2-positive breast cancer cells and tumor tissues, and monitors the dynamic downregulation of HER2 expression. WGYRGFYC rapidly distributes to target tissues and is efficiently cleared from non-target tissues via the kidneys, generating an ideal tumor-to-background ratio in imaging; it is a component of the PET radiotracer Ga-DOTA-WC8. WGYRGFYC exhibits no significant cytotoxicity in breast cancer cells, and can be used for non-invasive imaging diagnosis and therapeutic efficacy evaluation of HER2-positive breast cancer.

For research use only. We do not sell to patients.

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WGYRGFYC

WGYRGFYC Chemical Structure

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Description

WGYRGFYC (WC8) is a selective HER2-targeting peptide that binds specifically to HER2 by mimicking the antigen-binding site of trastuzumab. The DOTA precursor of WGYRGFYC has a KD of 61.20 nM for HER2. WGYRGFYC enables specific and highly sensitive detection of HER2 expression in HER2-positive breast cancer cells and tumor tissues, and monitors the dynamic downregulation of HER2 expression. WGYRGFYC rapidly distributes to target tissues and is efficiently cleared from non-target tissues via the kidneys, generating an ideal tumor-to-background ratio in imaging; it is a component of the PET radiotracer Ga-DOTA-WC8. WGYRGFYC exhibits no significant cytotoxicity in breast cancer cells, and can be used for non-invasive imaging diagnosis and therapeutic efficacy evaluation of HER2-positive breast cancer[1].

IC50 & Target

HER2

 

In Vitro

DOTA-WC8 (39-625 nM) binds to HER2 with nanomolar affinity (Kd=61.20 nM) in cell-free SPR assays[1].
[68Ga]Ga-DOTA-WGYRGFYC (37 KBq; 2 h) binds to HER2 in SKBR3 cells, with an IC50 of 51.89 nM[1].
Treatment with 10 μM Pyrotinib reduces the uptake of [68Ga]Ga-DOTA-WGYRGFYC (37 KBq; 15-120 min) by SKBR3 cells, indicating downregulation of HER2 expression[1].

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

In Vivo

[68Ga]Ga-DOTA-WC8 (3.7 MBq; i.v.; single dose) specifically accumulates in HER2-positive SKBR3 tumors with a peak tumor-to-muscle ratio of 4.31 and sensitively detects reduced HER2 expression after pyrotinib treatment[1].
68Ga]Ga-DOTA-WC8 (3.7 MBq; i.v.; single dose) exhibits minimal accumulation in HER2-negative MDA-MB-231 tumors, confirming its HER2 specificity[1].
68Ga]Ga-DOTA-WC8 (i.v.; single dose) has favorable pharmacokinetics in normal mice with rapid distribution and clearance[1].

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

Animal Model: BALB/c nude (female, 4-5 weeks old)[1]
Dosage: 3.7 MBq
Administration: i.v.; single dose
Result: Exhibited a two-compartment pharmacokinetic profile with a distribution half-life (T1/2α) of 2.898 min and an elimination half-life (T1/2β) of 23.477 min.
Rapidly absorbed by target tumor tissues, while the remaining radiotracer is efficiently cleared from the bloodstream, resulting in an optimal tumor/background ratio (TBR) at early time points postinjection.
Molecular Weight

1051.18

Formula

C51H62N12O11S

Sequence

Trp-Gly-Tyr-Arg-Gly-Phe-Tyr-Cys

Sequence Shortening

WGYRGFYC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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WGYRGFYC
Cat. No.:
HY-P11590
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