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Anti-TGFB1 (Fresolimumab)-SPDB-DM4 ADC

Anti-TGFB1 (Fresolimumab)-SPDB-DM4 ADC (CAT#: ADC-W-1797)

This ADC product is comprised of an anti-TGFB1 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
TGFB1

Alternative Names
TGFB1; transforming growth factor, beta 1; DPD1, TGFB; transforming growth factor beta-1; Camurati Engelmann disease; CED; TGFbeta; TGF-beta-1; TGF-beta 1 protein; latency-associated peptide; LAP; DPD1; TGFB;

Target Entrez Gene ID
7040

Target UniProt ID
P01137

Overview
This gene encodes a secreted ligand of the TGF-beta (transforming growth factor-beta) superfamily of proteins. Ligands of this family bind various TGF-beta receptors leading to recruitment and activation of SMAD family transcription factors that regulate gene expression. The encoded preproprotein is proteolytically processed to generate a latency-associated peptide (LAP) and a mature peptide, and is found in either a latent form composed of a mature peptide homodimer, a LAP homodimer, and a latent TGF-beta binding protein, or in an active form consisting solely of the mature peptide homodimer. The mature peptide may also form heterodimers with other TGFB family members. This encoded protein regulates cell proliferation, differentiation and growth, and can modulate expression and activation of other growth factors including interferon gamma and tumor necrosis factor alpha. This gene is frequently upregulated in tumor cells, and mutations in this gene result in Camurati-Engelmann disease.

Overview
Human Anti-TGFB1 IgG4-kappa antibody, Fresolimumab

Generic name
Fresolimumab

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-1796	Anti-TGFB1 (Fresolimumab)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-1803	Anti-TGFB1 (Metelimumab)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
ADC-W-1805	Anti-TGFB1 (Metelimumab)-MC-Vc-PAB-MMAE ADC	MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)	MMAE
ADC-W-1804	Anti-TGFB1 (Metelimumab)-MC-MMAF ADC	MC (maleimidocaproyl)	MMAF
ADC-W-1801	Anti-TGFB1 (Fresolimumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC	MC-Vc-PAB-DMEA-(PEG2)	duocarmycin SA

CAT#	Product Name	Linker	Payload
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-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-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-2590	Anti-EGFR (Cetuximab)-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)

CAT#	Product Name	Linker	Payload
ADC-W-2595	Anti-ERBB2 (Trastuzumab)-SPDB-DM4 ADC	SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)	DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
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-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-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-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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