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ERBB2
Anti-ERBB2-SPP-DM1 ADC

Anti-ERBB2-SPP-DM1 ADC (CAT#: ADC-W-605)

This ADC product is comprised of an anti-ERBB2 monoclonal antibody conjugated via a SPP linker to DM1. The DM1 is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, DM1 binds to tubulins, interrupts microtubule dynamics, and subsequently, induces cell death.

ADC Target
ADC Antibody
ADC Linker
ADC payload drug

Name
ERBB2

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 1

Target Entrez Gene ID
2064

Target UniProt ID
P04626

Overview
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.

Overview
Humanized Anti-ERBB2 lgG1 Antibody

Species Reactivity
Human

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

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.

Name
DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)

Description
Derived from Maytansinoid,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.

For Research Use Only. NOT FOR CLINICAL USE.

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Scientific Resources

CAMouse™-Fully Human Antibody Generation Platform

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Same Target Same Linker Same Payload

CAT#	Product Name	Linker	Payload
ADC-W-1112	Anti-ERBB2 (Pertuzumab)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-1114	Anti-ERBB2 (Pertuzumab)-MC-MMAF ADC	MC (maleimidocaproyl)	MMAF
ADC-W-2597	Anti-ERBB2 (Trastuzumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC	MC-Vc-PAB-DMEA-(PEG2)	duocarmycin SA
ADC-W-1113	Anti-ERBB2 (Pertuzumab)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-1110	Anti-ERBB2 (Margetuximab)-MC-Vc-PAB-SN38 ADC	MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)	SN-38 (7-ethyl-10-hydroxycamptothecin)

CAT#	Product Name	Linker	Payload
ADC-W-230	Anti-MUC1 ( huC242)-SPP-DM1 ADC	SPP (N-succinimidyl-4-(2-pyridyldithio)pentanoate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-226	Anti-ITIH4-SPP-DM1 ADC	SPP (N-succinimidyl-4-(2-pyridyldithio)pentanoate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-222	Anti-CD79b (SN8)-SPP-DM1 ADC	SPP (N-succinimidyl-4-(2-pyridyldithio)pentanoate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-597	Anti-NCAM1 (clone huN901)-SPP-[3H]DM1 ADC	SPP (N-succinimidyl-4-(2-pyridyldithio)pentanoate)	[3H]DM1([3H]N2'-deacetyl-N2'-(3-mercapto-1-oxopropyl)-maytansine)
ADC-W-617	Anti-MS4A1-SPP-DM1 ADC	SPP (N-succinimidyl-4-(2-pyridyldithio)pentanoate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)

CAT#	Product Name	Linker	Payload
ADC-W-572	Anti-ERBB2 (Trastuzumab-Fab)-SPP-DM1 ADC	SPP (N-succinimidyl-4-(2-pyridyldithio)pentanoate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-AA-015	anti-HIgG(Fc)Fab-N-DM1 ADC	Noncleavable linkers	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-AA-026	anti-MIgG(Fc)-N-DM1 ADC	Noncleavable linkers	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-460	Anti-NCAM1 (clone huN901)-SPP-DM1 ADC	SPP (N-succinimidyl-4-(2-pyridyldithio)pentanoate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-603	Anti-FOLH1 (clone J591)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)

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