小分子抑制剂

Small molecule inhibitor

Trastuzumab

货号:HY-P9907
规格:
名称:Synonyms: 曲妥珠单抗; Anti-Human HER2, Humanized Antibody

产品详情

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.

IC50 & Target[1]

HER2

体外研究
(In Vitro)

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].

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

体内研究
(In Vivo)

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].

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

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT04158258 Hoffmann-La Roche|Latin American Cooperative Oncology Group
Breast Cancer
February 21, 2020  
NCT02774681 Northwestern University|Pfizer|National Cancer Institute (NCI)
Breast Carcinoma Metastatic in the Brain|Estrogen Receptor Negative|HER2+Neu Negative|HER2+Neu Positive|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IV Breast Cancer
August 31, 2016 Phase 2
NCT03493854 Hoffmann-La Roche
Early Breast Cancer
June 14, 2018 Phase 3
 
分子量

145531.50

Formula

C6470H10012N1726O2013S42

CAS 号
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.

参考文献