2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Antibody-drug Conjugate/ADC Related
  3. Radionuclide-Drug Conjugates (RDCs) EGFR ADC Antibody
  4. Trastuzumab

Trastuzumab  (Synonyms: 曲妥珠单抗; Anti-Human HER2, Humanized Antibody)

目录号: HY-P9907 纯度: 99.80%
COA

摩尔计算器

Trastuzumab 是一种人源化 IgG1 单克隆抗体，其以高亲和力与 HER2 选择性结合。Trastuzumab 可用于 HER2 阳性转移性乳腺癌和 HER2 阳性胃癌 的研究。

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CAS No. : 180288-69-1

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Other Forms of Trastuzumab:

Trastuzumab 相关抗体

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

同型

Human IgG1 kappa
推荐同型对照抗体
种属

Humanized
IC50 & Target[1]

RDC Antibody

 

HER2

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MOLT-4 IC50
3.25 μM
Compound: 1a
Cytotoxic effect on the growth of human T-and B-lymphoblastoid cell lines(MOLT-4 and MGL-8) evaluated by measuring inhibition of thymidine intake in presence of 10 uM deoxyguanosine
Cytotoxic effect on the growth of human T-and B-lymphoblastoid cell lines(MOLT-4 and MGL-8) evaluated by measuring inhibition of thymidine intake in presence of 10 uM deoxyguanosine
[PMID: 1573639]
体外研究
(In Vitro)

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.

Trastuzumab 相关抗体:
体内研究
(In Vivo)

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.
Clinical Trial
CAS 号
性状

固体

颜色

White to light yellow

中文名称

曲妥珠单抗；曲妥单抗；群司珠单抗
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
Format
  • Human IgG1 kappa
Biological Activity
  • 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.
  • 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.
  • 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.
  • Immobilized HER2/CD340 Protein, Human (630a.a, HEK293, His, HY-P70254) can bind Trastuzumab.The EC50 for this effect is 2.16 ng/mL.
纯度 & 产品资料

纯度: 99.80%

COA (264 KB)

抗体抑制剂使用指南 (1152 KB)
参考文献
Cell Assay
[3]

The effects of Trastuzumab and Trastuzumab-F(ab′)2 on the growth of JIMT-1, SKBR-3, and BT-474 cells are evaluated using the AlamarBlue method. Exponentially growing cells are harvested and plated in single wells of a 96-well flat-bottomed tissue culture plate at defined densities, ranging from 4,500-8,000 cells per well depending on the cell line. After overnight culture, the regular medium is exchanged to medium containing 0, 1, 10, or 100 μg/mL Trastuzumab or Trastuzumab-F(ab′) 2. Cell viability is tested after 72 h of treatment. Fluorescence is detected at an excitation of 544 nm, and emission is detected at 590 nm[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Trastuzumab and Trastuzumab-F(ab′)2 are given at a dose of 5 and 25 μg/g, respectively, by weekly i.p. injection. The five times greater amount of administered F(ab′)2 is chosen based on the different half-lives of IgG and F(ab′) F(ab′)2. Control mice are treated with weekly i.p. injection of 100 μL physiologic saline (saline). Animals are euthanized by CO2 inhalation[3].

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

Trastuzumab 相关分类

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  • 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.

Keywords:

Trastuzumab180288-69-1Anti-Human HER2, Humanized Antibody曲妥珠单抗曲妥单抗群司珠单抗Radionuclide-Drug Conjugates (RDCs)EGFRADC AntibodyEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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