Trastuzumab (anti-HER2)  (Synonyms: Anti-Human HER2, Humanized Antibody (PBS))

Trastuzumab (PBS) is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab (PBS) has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.

Human IgG1 kappa

Human IgG1 kappa, Isotype Control

Humanized

用 Trastuzumab 处理过表达 HER2 的乳腺癌细胞系会导致 p27KIP1 和 Rb 相关蛋白 p130 的诱导，从而显著减少经历 S 期的细胞数量。由于 Trastuzumab 与 HER2 过表达细胞结合，在体外观察到许多其他表型变化。Trastuzumab 通过其人免疫球蛋白 G1 Fc 结构域与人体免疫系统相互作用可能会增强其抗肿瘤活性。体外研究表明，Trastuzumab 在介导抗体依赖性细胞介导的针对 HER2 过表达肿瘤靶标的细胞毒性方面非常有效^[1]。Trastuzumab 由两个抗原特异性位点组成，它们结合 HER2 受体胞外结构域的近膜部分，并阻止其胞内酪氨酸激酶的激活。Trastuzumab 募集负责抗体依赖性细胞毒性的免疫效应细胞^[2]。Trastuzumab IgG 的存在显著增加了对所有乳腺癌细胞系的杀伤力。Trastuzumab 诱发的 PBMC 的 ADCC 活性对 Trastuzumab 敏感 (SKBR-3) 或 Trastuzumab 耐药 (JIMT-1) 乳腺癌细胞同样很强，剂量依赖性细胞死亡在效应物/靶标处达到 50-60%，杀死比例为 60:1^[3]。

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

小鼠异种移植模型的 Trastuzumab 处理可显著抑制肿瘤生长。当与标准细胞毒性化疗药物联合使用时，Trastuzumab 处理与单独使用任一药物相比通常具有统计学上更好的抗肿瘤疗效^[1]。Trastuzumab 可显著抑制裸鼠和 SCID 小鼠肉眼可见的 JIMT-1 异种移植肿瘤的生长^[3]。

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

180288-69-1

液体

Colorless to light yellow

Shipping with dry ice.

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

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  Human IgG1 kappa

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  Loaded Her2/CD340 Protein, Human (Biotinylated, HEK293, His, HY-P78882) on AHC2 biosensor, can bind Trastuzumab with an affinity constant of 6.903E-10 M as determined in BLI assay.
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  Trastuzumab has a significant ADCC effect on BT474 cells in a dose-dependent manner.The EC₅₀ for this effect is 26.36 and 32.09 ng/mL.
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  Trastuzumab has a significant ADCC effect on SK-BR-3 cells in a dose-dependent manner.The EC₅₀ for this effect is 14.43 and 16.70 ng/mL.

• [1]. Sliwkowski MX, et al. Nonclinical studies addressing the mechanism of action of trastuzumab. Semin Oncol. 1999 Aug;26(4 Suppl 12):60-70.  [Content Brief]

  [2]. Hudis CA, et al. Trastuzumab--mechanism of action and use in clinical practice. N Engl J Med. 2007 Jul 5;357(1):39-51.  [Content Brief]

  [3]. Barok M, et al. Trastuzumab causes antibody-dependent cellular cytotoxicity-mediated growth inhibition of submacroscopic JIMT-1 breast cancer xenografts despite intrinsic drug resistance. Mol Cancer Ther. 2007 Jul;6(7):2065-72.  [Content Brief]