1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. WGYRGFYC

WGYRGFYC (WC8) 是 HER2 的选择性靶向肽,通过模拟曲妥珠单抗的抗原结合位点与 HER2 特异性结合。WGYRGFYC 的 DOTA 前体对 HER2 的 KD 为 61.20 nM。WGYRGFYC 能够对 HER2 阳性乳腺癌细胞及肿瘤组织中的 HER2 表达进行特异性、高灵敏性检测,监测 HER2 表达的动态下调。WGYRGFYC 可快速分布至靶组织并从非靶组织经肾脏高效清除,在成像中可产生理想的肿瘤与背景比值,是 PET 放射性示踪剂 Ga-DOTA-WC8 的组分之一。WGYRGFYC 在乳腺癌细胞中无显著细胞毒性,可用于 HER2 阳性乳腺癌的非侵入性成像诊断、疗效评估[1]。

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Custom Peptide Synthesis

WGYRGFYC

WGYRGFYC Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

DOTA-WC8 (39-625 nM) 在无细胞 SPR 实验中以纳摩尔级亲和力 (Kd=61.20 nM) 结合 HER2[1]
68Ga]Ga-DOTA-WGYRGFYC (37 KBq;2 h) 可与 SKBR3 细胞中的 HER2 结合,其 IC50为 51.89 nM[1]
10 μM Pyrotinib 处理可降低 SKBR3 细胞对 [68Ga]Ga-DOTA-WGYRGFYC (37 KBq;15-120 min) 的摄取,表明 HER2 表达下调[1]

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

体内研究
(In Vivo)

[68Ga]Ga-DOTA-WC8 (3.7 MBq;静脉注射;单剂量) 可在 HER2 阳性 SKBR3 肿瘤中特异性聚集,其肿瘤与肌肉的峰值比值为 4.31±0.32,并且能灵敏检测吡咯替尼治疗后 HER2 表达的降低情况[1]
[68Ga]Ga-DOTA-WC8 (3.7 MBq;静脉注射;单剂量) 在 HER2 阴性的 MDA-MB-231 肿瘤中的摄取量极低,证实了其 HER2 特异性[1]
[68Ga]Ga-DOTA-WC8 (静脉注射;单剂量) 在正常小鼠体内具有良好的药代动力学特征,表现为快速分布与清除[1]

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.
分子量

1051.18

Formula

C51H62N12O11S

Sequence

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

Sequence Shortening

WGYRGFYC

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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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产品名称:
WGYRGFYC
目录号:
HY-P11590
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