ADCs Cytotoxin

ADCs Cytotoxin

Catalog Product Name CAS Number Molecular Formula Molecular Weight
BADC-00190 10-Deacetyl-7-xylosyl Paclitaxel 90332-63-1 C50H57NO17 943.98
BADC-00042 Daunorubicin 20830-81-3 C27H29NO10 527.52
BADC-00798 Actinomycin D 50-76-0 C62H86N12O16 1255.44
BADC-00801 Epirubicin 56420-45-2 C27H29NO11 543.52
BADC-00253 Cynaroside 5373-11-5 C21H20O11 448.39
BADC-00316 Rutin 153-18-4 C27H30O16 610.53
BADC-00072 Solasodine 126-17-0 C27H43O2N 413.64
BADC-00036 Triptolide 38748-32-2 C20H24O6 360.4
BADC-00228 Albendazole 54965-21-8 C12H15N3O2S 265.33
BADC-00192 Leiurotoxin-1 116235-63-3 C142H237N45O39S7 3424.1
BADC-00173 Phencarol 10447-39-9 C20H23NO.HCl 329.86
BADC-00191 ω-agatoxin-IVA 145017-83-0 C217H360N68O60S10 5202.48
BADC-00172 omega conotoxin MVIIA 107452-89-1 C102H172N36O32S7 2639.2
BADC-00724 α-amanitin 23109-05-9 C39H54N10O14S 918.97
BADC-00328 Topotecan 123948-87-8 C23H23N3O5 421.45
BADC-00267 Gossypol Acetic Acid 12542-36-8 C32H34O10 578.61
BADC-00359 Temechine hydrobromide 30015-57-7 C11H21N .HBr 248.2
BADC-00302 Noscapine 128-62-1 C22H23NO7 413.42
BADC-00358 MCD Peptide 32908-73-9 C110H192N40O24S4 2587.22
BADC-00799 Streptonigrin 3930-19-6 C25H22N4O8 506.46

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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