Traditional Cytotoxic Agents

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Traditional Cytotoxic Agents

Catalog Product Name CAS Number
BADC-00837 Methotrexate disodium 7413-34-5
Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibitin...
BADC-00037 Methotrexate 59-05-2
Methotrexate(WR19039; CL14377) can interfere with the growth of certain cells of the body, especially cells that reproduce quickly, such as cancer cells, bone marrow cells, and skin cells.
BADC-00184 Tubulysin A 205304-86-5
Tubulysin A is a novel antibiotic, which exhibits anti-microtubule, anti-mitotic, apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative activity. Tubulysins show very high cytotoxic ac...
BADC-00325 Paclitaxel 33069-62-4
Paclitaxel is a compound with anti-tumor activity extracted from the Pacific yew tree Taxus brevifolia. Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.
BADC-00842 Rebeccamycin 93908-02-2
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein k...
BADC-00190 10-Deacetyl-7-xylosyl Paclitaxel 90332-63-1
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative with improved pharmacological features and higher water solubility.
BADC-00840 Hygrolidin 83329-73-1
Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and ab...
BADC-00839 Mensacarcin 808750-39-2
Mensacarcin is a bacterial metabolite that has been found in S. bottropensis and has anticancer activity. It is cytostatic in the NCI-60 panel of cancer cell lines and cytotoxic to HepG2, HM02, KATO I...
BADC-00838 17-AEP-GA 75747-23-8
17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
BADC-00834 Aminohexylgeldanamycin 485395-71-9
Aminohexylgeldanamycin (AHGDM), a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin shows antiangiogenic and antitumor activities.
BADC-00831 Telomestatin 265114-54-3
Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. Telomestatin selectively facilitates the formation of intramolecular G-quadruplexes, in part...
BADC-00830 17-GMB-APA-GA 256337-10-7
17-GMB-APA-GA is an ADC Cytotoxin. 17-GMB-APA-GA is a potent HSP90 inhibitor and used for latent T. gondii infection research.
BADC-00869 AcLysValCit-PABC-DMAE-SW-163D 2411007-69-5
AcLysValCit-PABC-DMAE-SW-163D is a drug-linker conjugates for ADC which consists of a natural bis-intercalator, SW-163D, conjugated via an AcLysValCitPABC-DMAE linker.
BADC-00035 Taltobulin trifluoroacetate 228266-41-9
Taltobulin trifluoroacetate (HTI-286; SPA-110) is an analogue of Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin.
BADC-00034 Taltobulin 228266-40-8
Taltobulin, also known as HTI-286 and SPA-110, is a fully synthetic analog of the natural tripeptide hemiasterlin, inhibits tubulin polymerization and circumvents transport-based resistance to taxanes...
BADC-00823 ε-Amanitin 21705-02-2
ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II.
BADC-00860 Mal-PEG2-VCP-Eribulin 2130869-18-8
Mal-PEG2-VCP-Eribulin consists the ADCs linker (Mal-PEG2-VCP) and Eribulin. Eribulin is a mechanistically unique microtubule inhibitor for cancer. Mal-PEG2-VCP-Eribulin is an Eribulin-based drug for a...
BADC-00822 γ-Amanitin 21150-23-2
γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin (HY-19610) and β-Amanit...
BADC-00821 β-Amanitin 21150-22-1
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be us...
BADC-00859 DGN549-C 2058075-34-4
DGN549-C consists a cleavable ADC linker valine-alanine (va) and PBD dimer. DGN549 is a novel DNA-alkylating cytotoxic payload and can be used in the synthesis of antibody-drug conjugates (ADCs).

As a representative of the development direction of the new generation of antibody technology, antibody drug conjugates (ADCs) have high specificity of antibodies and high toxicity of cytotoxic drugs to tumors. Cytotoxic Agents play an anti-tumor role in ADCs, which can affect the expected efficacy of target tumors. Its chemical structure, coupling mode and coupling number also affect the biological activity of the antibody. In theory, cytotoxic substances such as chemotherapeutic drugs, toxins and radionuclides that have great killing effects on tumor cells can be used as cytotoxic molecules of ADCs.

Chemical characteristics and mechanism of action

The choice of cytotoxins is crucial for ADCs. The cytotoxin used for coupling must have clear mechanism of action, small molecular weight, high activity, and no immunogenicity, and they can still retain anti-tumor activity after chemically coupled to the antibody. At present, the mechanism of anticancer drugs used in clinic is mostly to interfere with or block the proliferation of cells.  According to the mechanism, it can be roughly divided into four categories.

  • Inhibition of DNA synthesis. The main structural characteristics of this anticancer drugs are as follows: containing a pyrimidine or heterocyclic compound similar to pyrimidine, and a glucose analogue with five-membered ring. It interferes with DNA synthesis by blocking the synthesis and exchange of deoxypurine nucleosides or deoxypyrimidine nucleosides. Such as, 5-Fluorouracil, which mainly exerts anticancer effects through antimetabolic effects.
  • Destruction of DNA structure or DNA synthesis. Anticancer drugs that directly destroy DNA structures or synthesize DNA are mostly alkylating agents and anticancer antibiotics. The structure and function of DNA are destroyed by cross-linking with DNA through alkylation. For example, nitrogen mustard alkylating agent betamerphalan mainly exerts anticancer effect through alkylation.
  • Inhibition of protein synthesis. Most of these drugs contain antifolate whose core is a pyrrole or pyrazine pyrimidine group, which affect the normal replication process of proteins by destroying the activity of intracellular folate reductase, thus inhibiting the growth of tumors.  Such as, pemetrexed disodium and methotrexate.
  • Inhibition of cell mitosis. These anticancer drugs are mainly characterized by multi-hydroxyl and multi-thick ring structural. Alkaloids derived from plants account for the majority of active ingredients. Such as, vincristine and vindesine.

Application

The selection of cytotoxic is very wide. In principle, compounds with high enough inhibitory activity against tumor cells can be used as coupling drugs. At present, the most cytotoxic used in ADCs are Auristatins, Maytansine and Calicheamicins. 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). Among them, Auristatin is dominating the market, accounting for more than 50% of ADC drugs under investigation.

References

  1. Hamilton, G.S. Antibody-drug conjugates for cancer therapy: The technological and regulatory challenges of developing drug-biologic hybrids. Biologicals, 2015, 43: 318-332.
  2. Dan, N.; et al. Antibody-Drug Conjugates for Cancer Therapy: Chemistry to Clinical Implications. Pharmaceuticals, 2018, 11: 32.
* Only for research. Not suitable for any diagnostic or therapeutic use.

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