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TNFRSF9
Anti-TNFRSF9 (Urelumab)-SMCC-DM1 ADC

Anti-TNFRSF9 (Urelumab)-SMCC-DM1 ADC (CAT#: ADC-W-1892)

This ADC product is comprised of an anti-TNFRSF9 monoclonal antibody conjugated via a SMCC 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
TNFRSF9

Alternative Names
TNFRSF9; tumor necrosis factor receptor superfamily, member 9; ILA; tumor necrosis factor receptor superfamily member 9; 4 1BB; CD137; CD137 antigen; T cell antigen ILA; T-cell antigen ILA; 4-1BB ligand receptor; homolog of mouse 4-1BB; receptor protein 4-1BB; T-cell antigen 4-1BB homolog; induced by lymphocyte activation (ILA); interleukin-activated receptor, homolog of mouse Ly63; 4-1BB; CDw137; MGC2172; FLJ43501;

Target Entrez Gene ID
3604

Target UniProt ID
Q07011

Overview
The protein encoded by this gene is a member of the TNF-receptor superfamily. This receptor contributes to the clonal expansion, survival, and development of T cells. It can also induce proliferation in peripheral monocytes, enhance T cell apoptosis induced by TCR/CD3 triggered activation, and regulate CD28 co-stimulation to promote Th1 cell responses. The expression of this receptor is induced by lymphocyte activation. TRAF adaptor proteins have been shown to bind to this receptor and transduce the signals leading to activation of NF-kappaB.

Overview
Human Anti-TNFRSF9 IgG4-kappa antibody, Urelumab

Generic name
Urelumab

Host animal
Human

Name
SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)

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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Same Target Same Linker Same Payload

CAT#	Product Name	Linker	Payload
ADC-W-1894	Anti-TNFRSF9 (Urelumab)-MC-MMAF ADC	MC (maleimidocaproyl)	MMAF
ADC-W-1897	Anti-TNFRSF9 (Urelumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC	MC-Vc-PAB-DMEA-(PEG2)	duocarmycin SA
ADC-W-1895	Anti-TNFRSF9 (Urelumab)-MC-Vc-PAB-MMAE ADC	MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)	MMAE
ADC-W-1893	Anti-TNFRSF9 (Urelumab)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-1896	Anti-TNFRSF9 (Urelumab)-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-582	Anti-ERBB2-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-495	Anti-EGFR (J2898A)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-2571	Anti-SLC34A2 (Lifastuzumab )-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-496	Anti-EGFR-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-2604	Anti-ITGB3 (Tadocizumab)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)

CAT#	Product Name	Linker	Payload
ADC-W-2532	Anti-CD22 (Pinatuzumab)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-2604	Anti-ITGB3 (Tadocizumab)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-2583	Anti-EGFR (Zalutumumab)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-2589	Anti-EGFR (Cetuximab)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-2521	Anti-CD22 (Inotuzumab)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)

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