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Anti-CTLA4 (Ticilimumab)-SPDB-DM4 ADC

Anti-CTLA4 (Ticilimumab)-SPDB-DM4 ADC (CAT#: ADC-W-1005)

This ADC product is comprised of an anti-CTLA4 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
CTLA4

Alternative Names
CTLA4; cytotoxic T-lymphocyte-associated protein 4; celiac disease 3 , CELIAC3; cytotoxic T-lymphocyte protein 4; CD; CD28; CD152; GSE; ICOS; CD152 isoform; celiac disease 3; cytotoxic T-lymphocyte antigen 4; cytotoxic T-lymphocyte-associated antigen 4; cytotoxic T-lymphocyte-associated serine esterase-4; cytotoxic T lymphocyte associated antigen 4 short spliced form; ligand and transmembrane spliced cytotoxic T lymphocyte associated antigen 4; GRD4; CTLA-4; IDDM12; CELIAC3;

Target Entrez Gene ID
1493

Target UniProt ID
P16410

Overview
This gene is a member of the immunoglobulin superfamily and encodes a protein which transmits an inhibitory signal to T cells. The protein contains a V domain, a transmembrane domain, and a cytoplasmic tail. Alternate transcriptional splice variants, encoding different isoforms, have been characterized. The membrane-bound isoform functions as a homodimer interconnected by a disulfide bond, while the soluble isoform functions as a monomer. Mutations in this gene have been associated with insulin-dependent diabetes mellitus, Graves disease, Hashimoto thyroiditis, celiac disease, systemic lupus erythematosus, thyroid-associated orbitopathy, and other autoimmune diseases.

Overview
Human Anti-CTLA4 IgG2 antibody, Ticilimumab

Generic name
Ticilimumab

Host animal
Human

Species Reactivity
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-1008	Anti-CTLA4 (Ticilimumab)-MC-Vc-PAB-SN38 ADC	MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)	SN-38 (7-ethyl-10-hydroxycamptothecin)
ADC-W-1000	Anti-CTLA4 (Ipilimumab)-MC-MMAF ADC	MC (maleimidocaproyl)	MMAF
ADC-W-1007	Anti-CTLA4 (Ticilimumab)-MC-Vc-PAB-MMAE ADC	MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)	MMAE
ADC-W-1002	Anti-CTLA4 (Ipilimumab)-MC-Vc-PAB-SN38 ADC	MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)	SN-38 (7-ethyl-10-hydroxycamptothecin)
ADC-W-1009	Anti-CTLA4 (Ticilimumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC	MC-Vc-PAB-DMEA-(PEG2)	duocarmycin SA

CAT#	Product Name	Linker	Payload
ADC-W-2621	Anti-NCAM1 (Lorvotuzumab )-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)
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-469	Anti-CA6 (clone huDS6)-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-2616	Anti-MS4A1-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)
ADC-W-469	Anti-CA6 (clone huDS6)-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-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)

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