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ERBB3
Anti-ERBB3 (Duligotumab)-SPDB-DM4 ADC

Anti-ERBB3 (Duligotumab)-SPDB-DM4 ADC (CAT#: ADC-W-2241)

This ADC product is comprised of an anti-ERBB3 monoclonal antibody conjugated via a SPDB linker to DM4. The DM4 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
ERBB3

Alternative Names
ERBB3; v-erb-b2 erythroblastic leukemia viral oncogene homolog 3 (avian); LCCS2, lethal congenital contracture syndrome 2; receptor tyrosine-protein kinase erbB-3; HER3; proto-oncogene-like protein c-ErbB-3; tyrosine kinase-type cell surface receptor HER3; LCCS2; ErbB-3; c-erbB3; erbB3-S; MDA-BF-1; c-erbB-3; p180-ErbB3; p45-sErbB3; p85-sErbB3; MGC88033;

Target Entrez Gene ID
2065

Target UniProt ID
P21860

Overview
This gene encodes a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases. This membrane-bound protein has a neuregulin binding domain but not an active kinase domain. It therefore can bind this ligand but not convey the signal into the cell through protein phosphorylation. However, it does form heterodimers with other EGF receptor family members which do have kinase activity. Heterodimerization leads to the activation of pathways which lead to cell proliferation or differentiation. Amplification of this gene and/or overexpression of its protein have been reported in numerous cancers, including prostate, bladder, and breast tumors. Alternate transcriptional splice variants encoding different isoforms have been characterized. One isoform lacks the intermembrane region and is secreted outside the cell. This form acts to modulate the activity of the membrane-bound form. Additional splice variants have also been reported, but they have not been thoroughly characterized.

Overview
Human Anti-ERBB3 IgG antibody, Duligotumab

Generic name
Duligotumab

Host animal
Human

Name
SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)

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
DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)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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CAMouse™-Fully Human Antibody Generation Platform

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Same Target Same Linker Same Payload

CAT#	Product Name	Linker	Payload
ADC-W-1128	Anti-ERBB3 (Seribantumab)-MC-Vc-PAB-SN38 ADC	MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)	SN-38 (7-ethyl-10-hydroxycamptothecin)
ADC-W-1129	Anti-ERBB3 (Seribantumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC	MC-Vc-PAB-DMEA-(PEG2)	duocarmycin SA
ADC-W-2366	Anti-ERBB3 (Duligotuzumab)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-2244	Anti-ERBB3 (Duligotumab)-MC-Vc-PAB-SN38 ADC	MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)	SN-38 (7-ethyl-10-hydroxycamptothecin)
ADC-W-2243	Anti-ERBB3 (Duligotumab)-MC-Vc-PAB-MMAE ADC	MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)	MMAE

CAT#	Product Name	Linker	Payload
ADC-W-422	Anti-ITGAV (clone MF-T)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-2611	Anti-MS4A1 (Rituximab)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-516	Anti-FOLR1 (M9346A)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-095	Anti-LAMP1 (clone chMAbl)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-320	Anti-SDC1 (nBT062)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)

CAT#	Product Name	Linker	Payload
ADC-W-474	Anti-MSLN-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-2605	Anti-ITGB3 (Tadocizumab)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-516	Anti-FOLR1 (M9346A)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-422	Anti-ITGAV (clone MF-T)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-480	Anti-CD33 (huMy9-6)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)

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