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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C51H62N12O11S
- 分子量:1051.18
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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HER2 |
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.
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.
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Animal Model:BALB/c nude (female, 4-5 weeks old)[1]
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Dosage:3.7 MBq
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Administration:i.v.; single dose
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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.
化学情報
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分子量 1051.18
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分子式 C51H62N12O11S
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配列
Trp-Gly-Tyr-Arg-Gly-Phe-Tyr-Cys
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シーケンスの短縮
WGYRGFYC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)