ADC Cytotoxin are a large collection of toxins for antibody-drug conjugate (ADC) development projects. The toxins that can be used as payloads should be soluble, amenable to conjugation, and stable. There are myriads of cellular toxins in natural or synthesized, but only a few have been found adaptable for an ADC concept.
The toxins targeting tubulin ﬁlaments include Maytansinoids, Auristatins, Taxol derivatives, etc. Amatoxins are a class of transcription-inhibiting agents. They bind to RNA polymerase II, leading to cell apoptosis. Protein toxins function in the similar MOA (mechanism of action) with cellular toxins, they could inhibit protein synthesis and induce cell death. While enzyme-based ADCs alter the microenvironment of disease tissues to disturb their functions.
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Mafodotin, also known as mc-MMAF and SGD-1269 or Maleimidocaproyl monomethylauristatin F, is a MMAF derivative having a Maleimidocaproyl linker (MC linker), which is ready to conjugate to antibody or other proteins or biopolymers. Mafodotin is a useful agent for make antibody drug conjugate (ADC) for targeted drug delivery. MMAF is a potent antimitotic and antitublin auristatin derivative with a charged C-terminal phenylalanine residue that attenuates its cytotoxic activity compared to its uncharged counterpart, MMAE.
A highly potent metabolite of the anthracycline nemorubicin with outstanding cytotoxicity; a topoisomerase inhibitor and ADCs cytotoxin.
A potent tubulin inhibitor that is a toxin payload in antibody drug conjugates (ADCs).
Mertansine (DM1) is a tubulin inhibitor; thiol-containing maytansinoid that create an antibody-drug conjugate (ADC); an ADC payload.
SGD-1882 (PBD dimer, Pyrrolobenzodiazepine dimer) is a novel potent DNA-intercalating payload dimer (PBD dimer) payload for antibody-drug conjugates (ADCs).
Calicheamicin γ1 is an enediyne antitumor antibiotic that acts by binding to DNA and causes strand scission; ADC payload used in development of antibody drug conjugates.
An antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin. It is linked to an antibody with high affinity to structures on cancer cells, causing MMAF to accumulate in such cells; an ADC payload.
Ansamitocin P 3
A microtubule depolymerizing agent that can be isolated from culture broths of certain Gram-positive bacteria; binds tubulin (Kd=1.3 uM), depolymerizes microtubules in both interphase and mitosis, and perturbs chromosome segregation; inhibits the growth of cancer cells in culture and significantly suppresses the growth of several cancer tumors in mice.
Maytansinol (Ansamitocin P-0) is a microtubule assembly inhibitor; ADC payload in development of antibody drug conjugates.
Daun02 a prodrug that is converted by β-galactosidase to Daunorubicin, inactivate activated neurons that express both β-galactosidase and Fos, specifically attenuates cocaine-induced locomotor activity, also attenuates cocaine-induced β-galactosidase expression; daunorubicin, the active product of Daun02 metabolism by β-galactosidase, decreases the activity of MSNs in rat brain slices and that Daun02 strongly decreases the excitability of rat MSN primary cultures expressing β-galactosidase upon D1 dopamine receptor stimulation; Daun02-inactivation method, selectively inactivate only those neurons activated by cocaine in an environment repeatedly paired with drug injections.
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