ADCs Cytotoxin

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ADCs Cytotoxin

Catalog Product Name CAS Number
BADC-00274 Imperialine 61825-98-7
Imperialine is an isosteroidal alkaloid from Fritillaria thunbergii, a short-acting selective M2 muscarinic receptor antagonist.
BADC-00077 DL-Tetrahydroberberine 522-97-4
Tetrahydroberberine is a protoberberine alkaloid which potently block functional KATP channels natively expressed on midbrain dopamine neurons. Tetrahydroberberine is used for treatment of degenerativ...
BADC-00255 Deltaline 6836-11-9
Deltaline has a lycoctonine carbon-atom skeleton with four six-membered rings and three five-membered rings among; three of the six-membered rings adopt chair conformations with the fourth adopting a ...
BADC-00237 Artemisinin 63968-64-9
Artemisinin is a natural product originally isolated from plants of the genus Artemisia. It effectively kills malarial parasites of the genus Plasmodium. It is usually used in combination therapy for ...
BADC-00052 γ-Fagarine 524-15-2
γ-Fagarine is a natural compound extracted from Phellodendron chinense.
BADC-00267 Gossypol Acetic Acid 12542-36-8
Gossypol Acetic Acid is a phenol compound from plants of the Gossypium genus, Malvaceae. It binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively. It exhibits a...
BADC-00253 Cynaroside 5373-11-5
Cynaroside is a flavone, a flavonoid-like chemical compound. It is a 7-O-glucoside of luteolin.
BADC-00723 N-Acetyl-Calicheamicin 108212-76-6
N-Acetyl-Calicheamicin is a potent enediyne antitumor antibiotic that could be a potential cytotoxic DNA-binding agent in antibody-drug-conjugation (ADC). Calicheamicin is a naturally occurring hydrop...
BADC-00357 Ansamitocin P-3 66584-72-3
It is produced by the strain of Nocardia sp. C-15003(N-1). It has the function of anti-tumor, anti-plant pathogenic fungi, skin fungi and protozoa, and has no antibacterial activity.
BADC-00687 N-Me-L-Ala-maytansinol 77668-69-0
N-Me-L-Ala-maytansinol is a hydrophobic, cell permeable payload used in the preparation of antibody-drug conjugate (ADC).
BADC-00153 Chlorotoxin 163515-35-3
Chlorotoxin (Cltx) is a neurotoxin that was originally isolated from the venom of Leiurus quinquestriatus. Chlorotoxin is a specific ligand of glioma cells. Chlorotoxin binds to Cl- channels (small co...
BADC-00048 Charybdotoxin 95751-30-7
Charybdotoxin is a Ca2+-activated K+ channel blocker used as an ADC Cytotoxin.
BADC-00177 Graveoline 485-61-0
Graveoline isolated from ethanolic extract of Ruta graveolens triggers apoptosis and autophagy in skin melanoma cells: a novel apoptosis-independent autophagic signaling pathway.
BADC-00172 omega conotoxin MVIIA 107452-89-1
ω conotoxin MVIIA (omega conotoxin MVIIA) has been isolated from the venom of the cone Conus magus. Omega-conotoxins act at presynaptic membranes, they bind and block voltage-sensitive calcium channel...
BADC-00791 Illudin S 1149-99-1
Illudin S is a natural sesquiterpene agent with strong anti-tumour activity. Illudin S inhibits DNA synthesis via an unknown mechanism.
BADC-00775 FR-901464 146478-72-0
It is a potent cell cycle inhibitor isolated from Pseudomonas sp. No.2663. It exhibits potent antitumor activities against tumor cell lines via binding to the spliceosome and modulating pre-mRNA splic...
BADC-00707 Thailanstatin A 1426953-21-0
Thailanstatin A is a splicesosome inhibitor that acts via suppressing RNA-polymerase II. It is effective against cancers, and can be used as a payload for ADCs.
BADC-00189 Ansamitocin P 3' 66547-09-9
Ansamitocin P 3' is an isomer of Ansamitocin P-3, a potent anti-tumor maytansinoid antibiotic found in Actinosynnema pretiosum, a maytansine analog which displays potent cytotoxicity against the human...
BADC-00789 Leptomycin B 87081-35-4
a potent anti-fungal antibiotic. Leptomycin B is an inhibitor of export protein CRM1.
BADC-00088 Nemorubicin 108852-90-0
Nemorubicin, is a doxorubicin derivative that differs significantly from its parent drug in terms of spectrum of antitumor activity, metabolism and toxicity profile. The drug is active on tumors resis...

Antibody-drug conjugate (ADC) combines the high specificity of monoclonal antibody drugs with the high activity of small molecule cytotoxic drugs to improve the targeting of cancer drugs and reduce toxic side effects. The mechanism of action involves using monoclonal antibodies to specifically target cancer cells, and kill the cancer cells by coupled small molecule drugs.

ADCs Cytotoxin

Requirements for ADC linked toxins include: 1. Sufficient water solubility and stability in serum, because ADC may circulate in the body for several days; 2. Toxins must have functional groups that can be used to couple with the Linker;3. Toxins must be insensitive to enzymatic degradation reactions of lysosomes; 4. Toxins can reduce the aggregation effect (lipophilic substances tend to occur) and alter the interaction between ADC and pGp (permeability glycoprotein), which is the main cause of multipotent drug resistance (MDR) in tumor cells. In addition, for cleavable linker ADC, the side effect is that the toxin kills the target cells and then enters and exits the cell membrane to kill the surrounding cells. Such cleavable linker ADC requires a toxin with a certain lipid-water partition coefficient (LogP) and a positive / neutral charge.

Common toxins used in ADC drugs are extremely toxic and with little selectivity, which makes them difficult to use alone as small molecule drugs. These toxins have often been studied as chemical drugs in the past but have been abandoned due to their later emerged toxicity. At present, the most commonly used cytotoxic drugs can be divided into two categories according to their mechanism of action: (1) DNA damaging agents: these drugs act on calicheamicin (CLM, an alkene diyne antibacterial drug) of DNA, causing DNA cleavage and cell death by binding to the DNA double helix groove. (2) Tubulin inhibitors: by binding to microtubules, they prevent the polymerization of microtubules, block the cell cycle, and induce tumor cell apoptosis. Tubulin inhibitors can also be divided into two major categories: dolastatin and its auristatin derivatives (MMAE, MMAF, MMAD); and maytansin and maytansinoid derivatives (DM1, DM2, DM3, DM4). At present, majority of clinical research involving ADCs projects use tubulin inhibitors, and both subtoxoids have approved products on the market (Adcetris uses oristatin MMAE and Kadcyla uses maytansinoid DM1). Auristatin is dominating the market, accounting for more than 50% of ADC drugs under investigation.

References:

  1. Nirnoy Dan, Saini Setua, Vivek K. Kashyap.Antibody-Drug Conjugates for Cancer Therapy:Chemistry to Clinical Implications.Pharmaceuticals. 2018, 11, 32,1-22.
  2. Siler Panowksi,Sunil Bhakta,Helga Raab.Site-specific antibody drug conjugates for cancer therapy.Landes Bioscience.2014,6:1, 34–45.
* Only for research. Not suitable for any diagnostic or therapeutic use.

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