Anti-HER2 (trastuzumab)-SPP-DM1 ADC

Name: Anti-HER2 (trastuzumab)-SPP-DM1 ADC
SKU: ADC-135LCT
Rating: 5 (1 reviews)

CAT#: ADC-135LCT

This ADC product is composed of an anti-HER2 antibody (Trastuzumab) conjuagated via a SPP linker to DM1 (trastuzumab-SPP-DM1). It has demonstrated a response in breast, ovarian and lung cancer treatment by a MOA (Mechanism of Action) of Depolymerize Microtubules.

Gene Expression

Subcellular Location Figure 1 IF staining of human cell line U-251 MG

Immunofluorescent staining of human cell line U-251 MG shows localization to plasma membrane.

* Image credit: Image credit: Human Protein Atlas v21.proteinatlas.org/images/1060/169_D12_1_selected.jpg

Subcellular Location Figure 2 IF staining of human cell line A-431

Immunofluorescent staining of human cell line A-431 shows localization to plasma membrane.

* Image credit: Image credit: Human Protein Atlas v21.proteinatlas.org/images/1338/if_selected.jpg

Normal Tissue Figure 3 High expression in esophagus

* Image credit: Image credit: Human Protein Atlas v21.proteinatlas.org/images/1383/4682_B_5_1_val_selected.jpg

Normal Tissue Figure 4 IHC staining of human rectum

Immunohistochemical staining of human rectum shows weak cytoplasmic positivity in glandular cells.

* Image credit: Image credit: Human Protein Atlas v21.proteinatlas.org/images/43/ihc_selected.jpg

Normal Tissue Figure 5 IHC staining of human urinary bladder

Immunohistochemical staining of human urinary bladder shows moderate cytoplasmic and membranous positivity in urothelial cells.

* Image credit: Image credit: Human Protein Atlas v21.proteinatlas.org/images/20416/ihc_selected.jpg

Normal Tissue Figure 6 Kidney

Collecting ducts Staining: Low Intensity: Moderate Quantity: <25% Distal tubules Staining: Low Intensity: Moderate Quantity: <25%

* Image credit: Image credit: Human Protein Atlas v21.proteinatlas.org/images/43/1054_A_7_5.jpg

Normal Tissue Figure 7 Breast

Glandular cells Staining: Medium Intensity: Moderate Quantity: 75%-25% Location: Cytoplasmic/ membranous Myoepithelial cells Staining: Medium Intensity: Moderate Quantity: 75%-25% Location: Cytoplasmic/ membranous

* Image credit: Image credit: Human Protein Atlas v21.proteinatlas.org/images/20416/45831_B_3_4.jpg

RNA Expression Figure 8 RNA cell line category: Group enriched (OE19, SK-BR-3)

Cell lines ordered by descending RNA expression order

* Image credit: Image credit: Human Protein Atlas v21.proteinatlas.org/ENSG00000141736-ERBB2

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Specifications

Antibody Overview
Humanized (from Mouse) Anti-HER2

Clone
Trastuzumab

Linker
SPP (N-succinimidyl-4-(2-pyridyldithio)pentanoate)

Linker Class/Description
Disulfide Linkers are extensively exploited as a chemically labile linkage. Since the release of disulﬁde-linked drugs requires a cytoplasmic thiol cofactor, such as glutathione (GSH). Disulfides maintain stable at physiological pH and only when ADCs are internalized inside cells, the cytosol provides reducing environment including intracellular enzyme protein disulﬁde isomerase, or similar enzymes, drugs can be released.

Drug
DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)

Drug Class/Description
Maytansinoids are a group of cytotoxins structurally similar to rifamycin, geldanamycin, and ansatrienin. The eponymous natural cytotoxic agent maytansine is a 19-member lactam (ansa
macrolide) structure originally isolated from the Ethiopian shrub Maytenus ovatus. Maytansinoids can bind to tubulin at or near the vinblastine-binding site, which interfere the formation of microtubules and depolymerize already formed microtubules, inducing mitotic arrest in the intoxicated cells

Target

Introduction
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. [provided by RefSeq, Jul 2008]

Alternative Names
ERBB2; erb-b2 receptor tyrosine kinase 2; NEU; NGL; HER2; TKR1; CD340; HER-2; MLN 19; HER-2/neu; receptor tyrosine-protein kinase erbB-2; herstatin; p185erbB2; proto-oncogene Neu; c-erb B2/neu protein; proto-oncogene c-ErbB-2; metastatic lymph node gene 19 protein; human epidermal growth factor receptor 2; neuro/glioblastoma derived oncogene homolog; tyrosine kinase-type cell surface receptor HER2; neuroblastoma/glioblastoma derived oncogene homolog; v-erb-b2 avian erythroblastic leukemia viral oncoprotein 2; v-erb-b2 avian erythroblastic leukemia viral oncogene homolog 2; v-erb-b2 erythroblastic leukemia viral oncogene homolog 2, neuro/glioblastoma derived oncogene homolog;

Gene ID
2064

UniProt ID
P04626

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Related Diseases

Bladder Cancer

Non-small Cell Lung Cancer

Related Signaling Pathways

ErbB Signaling Pathway

Downloadable Resources

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Datasheet

Datasheet - ADC-135LCT.pdf

MSDS

MSDS - ADC-135LCT.pdf

COA

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