| 别名 | Herceptin，曲妥珠单抗 |
| 产品名 | Trastuzumab (Anti-Human HER2, Humanized Antibody) |
| CAS号 | 180288-69-1 |
| 目录号 | D802007 |
| 化学式 | C₆₄₇₀H₁₀₀₁₂N₁₇₂₆O₂₀₁₃S₄₂ |
| 分子量 | 145145.09 |
| 靶点 | <p>A monoclonal antibody with invasive breast cancers that overexpress HER2</p> |
| 储存条件 | Store at 4°C |
| 用途 | 仅供科学研究使用!不能用于人体及动物治疗 |
靶点及简介 ：
A monoclonal antibody with invasive breast cancers that overexpress HER2，
Trastuzumab (anti-HER2)曲妥珠单抗是人源重组的抗体抑制剂，与HER2的胞外区域相结合。 MW:145.53 KD。
Trastuzumab 可用于 HER2 阳性转移性乳腺癌和 HER2 阳性胃癌 的研究。
| CAS号 | 180288-69-1 |
|---|---|
| 配制 | PBS buffer, pH 7.2 |
| 同型 | Human IgG1 |
| 来源 | CHO cells |
| 储存条件 | Store the undiluted solution at 4°C in the dark to avoid freeze-thaw cycles |
体外研究：
Trastuzumab在过表达HER2的肿瘤细胞中发挥特异性抗肿瘤活性。Trastuzumab与HER2的近膜区结合，一旦与受体结合，这个抗体可下调HER2的表达。Trastuzumab选择性地抑制不依赖于配体的HER2-HER3二聚化。除此之外，trastuzumab与HER2结合可抑制HER2胞外区域的溶蛋白性裂解，导致p95-HER2水平降低。trastuzumab可导致PI3K信号通路和下游细胞周期进展相关介质如cyclin D1下调。Trastuzumab不仅抑制HER2信号通路，同时也在HER2过表达细胞中引起免疫相关反应。Trastuzumab的结合占用了免疫效应细胞上的Fc受体，导致抗体依赖性的细胞毒性。因此，trastuzumab具有抗血管生成的作用，降低化疗凋亡阈值。
Treatment of HER2-overexpressing breast cancer cell lines with Trastuzumab results in induction of p27KIP1 and the Rb-related protein, p130, which in turn significantly reduces the number of cells undergoing S-phase. A number of other phenotypic changes are observed in vitro as a consequence of Trastuzumab binding to HER2-overexpressing cells. Interaction of Trastuzumab with the human immune system via its human immunoglobulin G1 Fc domain may potentiate its antitumor activities. in vitro studies demonstrate that Trastuzumab is very effective in mediating antibody-dependent cell-mediated cytotoxicity against HER2-overexpressing tumor targets[1]. Trastuzumab consists of two antigen-specific sites that bind to the juxtamembrane portion of the extracellular domain of the HER2 receptor and that prevent the activation of its intracellular tyrosine kinase. Trastuzumab recruits immune effector cells that are responsible for antibody-dependent cytotoxicity[2]. The presence of Trastuzumab IgG significantly increases killing of all breast cancer cell lines. The ADCC activity of PBMCs evoked by Trastuzumab is equally strong against Trastuzumab-sensitive (SKBR-3) or Trastuzumab-resistant (JIMT-1) breast cancer cells, with dose-dependent cell death reaching 50–60% killing at an effector/target ratio of 60:1[3].
体内研究：
对一系列动物模型，包括灵长类动物，进行Trastuzumab的慢性给药，证明Trastuzumab是安全的。在模拟亚宏观疾病的辅助治疗实验中，trastuzumab能够抑制宏观上可检测的移植瘤的生长，可持续5-7周。Trastuzumab具有显著的抗肿瘤活性，目前正用于乳腺癌的治疗中。在体内模型中，trastuzumab降低乳腺癌移植瘤的微血管密度。Trastuzumab直接作用于癌细胞信号，间接地作用于免疫系统。
Trastuzumab treatment of mouse xenograft models results in marked suppression of tumor growth. When given in combination with standard cytotoxic chemotherapeutic agents, Trastuzumab treatment generally results in statistically superior antitumor efficacy compared with either agent given alone[1]. Trastuzumab causes a significant growth inhibition of the outgrowth of macroscopic JIMT-1 xenograft tumors in both nude and SCID mice[3].
验证：
参考文献：
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.0069 mL | 0.0344 mL | 0.0687 mL |
| 5 mM | 0.0014 mL | 0.0069 mL | 0.0137 mL |
| 10 mM | 0.0007 mL | 0.0034 mL | 0.0069 mL |
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