生物活性

Trastuzumab is a humanized 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

體外研究
(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. 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. 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.

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

reference only.

體內研究
(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. Trastuzumab causes a significant growth inhibition of the outgrowth of

macroscopic JIMT-1 xenograft tumors in both nude and SCID mice.

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

reference only.

分子量

145531.50

Formula

C₆₄70H₁₀012N₁₇₂6O₂₀13S₄₂

CAS 號

 180288-69-1

中文名稱

曲妥珠單抗；曲妥單抗；群司珠單抗