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Anti-C-kit (NEG087)-SMCC-DM1 ADC

Anti-C-kit (NEG087)-SMCC-DM1 ADC (CAT#: ADC-W-074)

This ADC product is comprised of an anti-C-kit monoclonal antibody (NEG087) 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
C-kit

Alternative Names
KIT; v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; PBT; SCFR; C-Kit; CD117; mast/stem cell growth factor receptor Kit; p145 c-kit; proto-oncogene c-Kit; piebald trait protein; soluble KIT variant 1; tyrosine-protein kinase Kit; proto-oncogene tyrosine-protein kinase Kit; v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene-like protein;

Target Entrez Gene ID
3815

Target UniProt ID
A0A024RDA0

Overview
This gene encodes the human homolog of the proto-oncogene c-kit. C-kit was first identified as the cellular homolog of the feline sarcoma viral oncogene v-kit. This protein is a type 3 transmembrane receptor for MGF (mast cell growth factor, also known as stem cell factor). Mutations in this gene are associated with gastrointestinal stromal tumors, mast cell disease, acute myelogenous lukemia, and piebaldism. Multiple transcript variants encoding different isoforms have been found for this gene.

Overview
Anti-C-kit antibody, NEG087

Generic name
NEG087

Species Reactivity
Human

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

Description
Noncleavable linkers, is considered noncleavable-meaning linker cleavage, and payload release does not depend on the differential properties between the plasma and some cytoplasmic compartments. Instead, the release of the cytotoxic drug is postulated to occur after internalization of the ADC via antigen-mediated endocytosis and delivery to lysosomal compartment, where the antibody is degraded to the level of amino acids through intracellular proteolytic degradation.

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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CAMouse™-Fully Human Antibody Generation Platform

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Same Linker Same Payload Same Target

CAT#	Product Name	Linker	Payload
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-457	Anti-MST1R (clone Zt/g4)-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-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-2589	Anti-EGFR (Cetuximab)-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-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-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-541	Anti-CD44 (clone BIWA 4)-DM1 ADC		DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-AA-050	Protein G-MCC-DM1 ADC	MCC (Maleimidomethyl cyclohexane-1-carboxylate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)

CAT#	Product Name	Linker	Payload
ADC-W-071	Anti-C-kit (NEG024)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-073	Anti-C-kit (NEG086)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-072	Anti-C-kit (20376)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-078	Anti-C-kit (9P3)-CX1-1-DM1 ADC	CX1-1 (2,5-dioxopyrrolidin-1-yl 17-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-5,8,11,14-tetraoxo-4,7,10,13-tetraazaheptadecan-1-oate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)
ADC-W-075	Anti-C-kit (NEG026)-SMCC-DM1 ADC	SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)	DM1 (N2’-Deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine)

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