Non-fucosylated Anti-Human HER2 (ado-trastuzumabemtansine) Therapeutic Antibody (CAT#: BioBet-006ZP) Datasheet

ERBB2

erb-b2 receptor tyrosine kinase 2

This gene encodes a member of the epidermal growth factor (EGF) receptor family of receptor tyrosine kinases. This protein has no ligand binding domain of its own and therefore cannot bind growth factors. However, it does bind tightly to other ligand-bound EGF receptor family members to form a heterodimer, stabilizing ligand binding and enhancing kinase-mediated activation of downstream signalling pathways, such as those involving mitogen-activated protein kinase and phosphatidylinositol-3 kinase. Allelic variations at amino acid positions 654 and 655 of isoform a (positions 624 and 625 of isoform b) have been reported, with the most common allele, Ile654/Ile655, shown here. Amplification and/or overexpression of this gene has been reported in numerous cancers, including breast and ovarian tumors. Alternative splicing results in several additional transcript variants, some encoding different isoforms and others that have not been fully characterized.

NEU; NGL; HER2; TKR1; CD340; HER-2; MLN 19; HER-2/neu

Plasma membrane, Endosome, Nucleus.

Diseases associated with ERBB2 include Glioma Susceptibility 1 and Gastric Cancer.

Its related pathways are Association Between Physico-Chemical Features and Toxicity Associated Pathways and RET signaling.

1.Protein tyrosine kinases are part of several cell surface receptor complexes, but obviously require a co-receptor to which a ligand binds. An essential component of the neurotonin receptor complex, although neurotonin does not interact with it alone. GP30 is a potential ligand for this receptor. Regulate the growth and stability of peripheral microtubules (MTs). After ERBB2 is activated, the memo1-rhoa-991 signaling pathway triggers the phosphorylation of GSK3B on the cell membrane, thereby inhibiting GSK3B. This prevents the phosphorylation of APC and CLASP2, allowing them to bind to the cell membrane. In turn, membrane-bound APC allows MACF1 to localize to the cell membrane, which is necessary for microtubule capture and stabilization. 2.Participate in transcriptional regulation in the nucleus. It is associated with the 5'-TCAAATTC-3' sequence in the PTGS2/COX-2 promoter and activates its transcription. Participate in CDKN1A transcriptional activation; functions include STAT3 and SRC. Participate in the transcription of rRNA genes through RNA Pol I, and promote protein synthesis and cell growth.

Cancer antibody; Controls and Markers antibody; Signaling Transduction antibody; Circulating Tumor Cells BioMarker antibody

Autophosphorylated. Autophosphorylation occurs in trans, i.e. one subunit of the dimeric receptor phosphorylates tyrosine residues on the other subunit (Probable). Ligand-binding increases phosphorylation on tyrosine residues (PubMed:27134172). Signaling via SEMA4C promotes phosphorylation at Tyr-1248 (PubMed:17554007). Dephosphorylated by PTPN12 (PubMed:27134172).

Protein Based Therapies
Monoclonal antibody (mAb)

IgG1

ado-trastuzumabemtansine

Mouse

Human

Trastuzumab emtansine is an antibody drug conjugate (ADC) consisting of the humanized monoclonal antibody trastuzumab (Herceptin) covalently linked to the cytotoxic agent DM1.

HER2-positive breast cancer; metastatic breast cancer; Refractory, metastatic Non small cell lung cancer

Ado-trastuzumab
Ado-trastuzumab emtansine
T-DM1
Trastuzumab emtansine
Trastuzumab-DM1
Trastuzumab-MCC-DM1

Trastuzumab Emtansine is a HER2 antibody drug conjugate. The antibody part is humanized anti-HER2 IgG1 trastuzumab, and the drug part is DM1, which is a maytansin derivative that inhibits microtubules. Emtansine is a generic name for 4- [N-maleimidomethyl] cyclohexane-1-carboxylic acid ester (MCC) covalently linking linker and DM1, which is produced through chemical synthesis. Trastuzumab Emtansine binds to subdomain IV of the HER2 receptor and enters the cell through receptor-mediated endocytosis. DM1 binds to tubulin in microtubules and inhibits microtubule function, resulting in cell arrest and apoptosis. Similarly, similar to trastuzumab, in vitro antibody-dependent cytotoxicity and inhibition of HER2 receptor signaling are mediated by the antibody portion of trastuzumab emtansine.

It is suitable for treating early HER2-positive early breast cancer or metastatic breast cancer that substantially overexpresses HER2. Approved for gastric cancer, metastatic gastroesophageal junction adenocarcinoma, and metastatic adenocarcinoma of the gastro-esophageal junction, provided that these cancers overexpress HER2.