Non-fucosylated Anti-Human HER2 Therapeutic Antibody, an ADCC-Enhanced Biobetter [Lot: CB20-PZ06] (CAT#: BioBet-006ZP) Datasheet

Target
HER2
Isotype
Whole Humanized Antibody
Description
ADCC-enhanced ado-trastuzumabemtansine is a non-fucosylated anti-HER2 therapeutic biobetter antibody. Creative Biolabs' Afuco™ technology platform allows for the control of glycosylation level, thereby achieving ADCC-Enhanced Anti-HER2 ado-trastuzumabemtansine, a biobetter by reducing fucosylation of the Fc region of ado-trastuzumabemtansine, leading to an increased binding affinity for the FcyR receptor on immune effector cells.
More specifically, the afucosylated therapeutic biobetter antibody was generated by recombinant DNA technology. It has been produced in CHO cells that are deficient for fucosylation and purified by affinity chromatography with protein G. The absence of the fucose residue from the N-glycans of IgG-Fc results in dramatic enhancement of antibody-dependent cellular cytotoxicity (ADCC).
Indication
HER2-positive breast cancer; metastatic breast cancer; Refractory, metastatic Non small cell lung cancer
Classification
Therapeutic antibody; Therapeutic antibody-drug conjugat; biobetter
Patent
Not Available
Status
Preclinical

Cooperation Seeking

Creative Biolabs is interested in collaborating with potential partners (include but not limit to major pharma or biotech firms) to further co-develop ADCC-enhanced ado-trastuzumab emtansine. For commercial partners interested in our ADCC-enhanced therapeutic antibodies, Creative Biolabs welcomes collaboration. Here are two ways for your choice, and please contact us for more details.
1) Collaborate with us and co-develop the programs from discovery phase to IND enabling. Costs will be shared.
2) Become a licensed candidate of our programs.
Looking forward to cooperating with you in the near future.
Official Name
ERBB2
Full Name
erb-b2 receptor tyrosine kinase 2
Background
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.
Alternative Names
NEU; NGL; HER2; TKR1; CD340; HER-2; MLN 19; HER-2/neu
Gene ID
UniProt ID
Cellular Localization
Plasma membrane, Endosome, Nucleus.
HGNC
OMIM
Involvement in Disease
Diseases associated with ERBB2 include Glioma Susceptibility 1 and Gastric Cancer.
Related Pathways
Its related pathways are Association Between Physico-Chemical Features and Toxicity Associated Pathways and RET signaling.
Function
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.
Field of research
Cancer antibody; Controls and Markers antibody; Signaling Transduction antibody; Circulating Tumor Cells BioMarker antibody
Post-translational modifications
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).
Trade name
Kadcyla
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Accession Number
DB05773
CAS number
1018448-65-1
Antibody Isotype
Whole Humanized Antibody
Antibody Clone
ado-trastuzumabemtansine
Description
Trastuzumab emtansine is an antibody drug conjugate (ADC) consisting of the humanized monoclonal antibody trastuzumab (Herceptin) covalently linked to the cytotoxic agent DM1. The United States Food and Drug Administration (FDA) approved trastuzumab emtansine for female patients with trastuzumab-resistant advanced HER2 positive breast cancer on February 22, 2013.
Indication
HER2-positive breast cancer; metastatic breast cancer; Refractory, metastatic Non small cell lung cancer
Synonyms
Ado-trastuzumab
Ado-trastuzumab emtansine
T-DM1
Trastuzumab emtansine
Trastuzumab-DM1
Trastuzumab-MCC-DM1
UNII
SE2KH7T06F

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.

All products and services are for Research Use Only. Do Not use in humans.

ONLINE INQUIRY

Creative Biolabs has established a team of customer support scientists ready to discuss ADCC/CDC optimization strategies, antibody production, bioinformatics analysis and other molecular biology/biotechnology issues.

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