Trastuzumab emtansine, formerly called Trastuzumab-DM1 (T-DM1) is a first-in-class HER2 antibody drug conjugate (ADC) comprised of Genentech's trastuzumab antibody linked to ImmunoGen's cell-killing agent, DM1. T-DM1 combines two strategies-- anti-HER2 activity and targeted intracellular delivery of the potent anti-microtubule agent, DM1 (a maytansine derivative)--to produce cell cycle arrest and apoptosis. Trastuzumab emtansine is marketed under the brand name Kadcyla and is indicated for use in HER2-positive, metastatic breast cancer patients who have already used taxane and/or trastuzumab for metastatic disease or had their cancer recur within 6 months of adjuvant treatment. The FDA label has two precautions. First that trastuzumab emtansine and trastuzumab cannot be interchanged. Second that there is a black box warning of serious side effects such as hepatotoxicity, embryo-fetal toxicity, and cardiac toxicity.

货号（Catalog No.）
CSD00241
通用名INN
Trastuzumab Emtansine
纯度(Purity)
>95%
浓度( Concentration)
1mg/ml
Formulation
PBS buffer pH7.5
Source
CHO cells
内毒素(Endotoxin level)
Please contact with the lab for this information.
生物活性
产品描述(Description)
Trastuzumab emtansine, formerly called Trastuzumab-DM1 (T-DM1) is a first-in-class HER2 antibody drug conjugate (ADC) comprised of Genentech's trastuzumab antibody linked to ImmunoGen's cell-killing agent, DM1. T-DM1 combines two strategies-- anti-HER2 activity and targeted intracellular delivery of the potent anti-microtubule agent, DM1 (a maytansine derivative)--to produce cell cycle arrest and apoptosis. Trastuzumab emtansine is marketed under the brand name Kadcyla and is indicated for use in HER2-positive, metastatic breast cancer patients who have already used taxane and/or trastuzumab for metastatic disease or had their cancer recur within 6 months of adjuvant treatment. The FDA label has two precautions. First that trastuzumab emtansine and trastuzumab cannot be interchanged. Second that there is a black box warning of serious side effects such as hepatotoxicity, embryo-fetal toxicity, and cardiac toxicity.
别名(Alternative names)
PRO132365,RG3502,T-DM1,trastuzumab-MCC-DM1
靶点;物种(Specificity target name;species)
ERBB2/EGFR2/CD340[Homo sapiens]
活性研究（体外/体内研究）(Activity in vitro)
PF299804对egfr信号传导有抑制作用，并可促使含EGFR T790M的H3255 GR细胞系凋亡。PF299804对表达t790m 突变体的h3255和 hcc827细胞的生长具有抑制作用。在HER2-扩增的胃癌细胞中，PF299804诱导细胞凋亡和G1期阻滞，并抑制HER家族及其下游信号通路，包括STAT3，AKT和细胞外信号调节激酶(ERK)中受体的磷酸化。PF299804还可阻断SNU216细胞中EGFR/HER2，HER2/HER3和HER3/HER4异质二聚体形成，以及HER3与p85α的结合。在大多数敏感细胞系中，PF299804对HER2，EGFR，HER4，AKT和ERK的磷酸化水平具有降低作用。PF299804通过G0/G1期阻滞和对细胞凋亡的诱导发挥其抗增殖作用。在47种人乳腺癌和永生的乳腺上皮细胞系中，相对于非扩增细胞系(RR = 3.39, p <0.0001)，PF299804优先抑制HER-2-扩增的乳腺癌细胞系的生长。
种类(Species)
Humanized
受体鉴定(Receptor identification)
IgG1-kappa
化学信息
CAS
1018448-65-1
存储条件(Storage)
store at -80°C
Note
For research use only. Not suitable for clinical or therapeutic use.