ADC Cytotoxin

Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and an IL receptor modulator. Dexamethasone has anti-inflammatory and immunosuppressive activity and induces autophagy. Dexamethasone inhibits LPS-induced inflammatory responses in macrophages.

Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I/II (IC50=0.8/2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.

Mertansine (DM1) refers to the thiol-containing maytansinoid, DM1 (N2'-deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine) attached to a monoclonal antibody through reaction of the thiol group with the SPP (N-succinimidyl 4-(2-pyridyldithio)) linker to create an antibody-drug conjugate or ADC. Experimental ADCs with the SPP-DM1 design include lorvotuzumab mertansine.

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.

Exatecan Mesylate (DX8951f) is a DNA topoisomerase I inhibitor (IC50: 2.2 μM, 0.975 μg/mL).

Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity. Camptothecin has antitumor activity and induces apoptosis.

7-Epi 10-desacetyl paclitaxel (10-Deacetyl-7-epipaclitaxel) shows IC50 values of 0.085 nM, against HeLa cells.

Aldoxorubicin hydrochloride is an albumin-binding prodrug of Doxorubicin, a DNA topoisomerase II inhibitor. Aldoxorubicin hydrochloride is released from albumin under acidic conditions. Aldoxorubicin hydrochloride exhibits potent antitumor activities in various cancer cell lines and in murine tumor models.

Taltobulin trifluoroacetate is a synthetic analogue of the tripeptide hemiasterlin, is a potent agent of antimicrotubule that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.

(4-NH2)-Exatecan is a topoisomerase inhibitor with potential anticancer activity for the synthesis of antibody drug conjugates (ADCs).

DRF-1042 is an orally active camptothecin analog with antitumor activity and inhibits DNA topoisomerase I. It is used in the study of refractory tumors.

Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM[1].

Aldoxorubicin has effective antitumor activities in various cancer cell lines and in murine tumor models. Aldoxorubicin is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitors).

Doxorubicin (Adriamycin) is a Topoisomerase II (Top2) inhibitor with antineoplastic activity.

Daunorubicin hydrochloride (Rubidomycin hydrochloride), an anthracycline aminoglycoside antineoplastic, inhibits DNA replication and repair and RNA and protein synthesis.

Eribulin (B1939) is a nonpaclitaxel microtubule kinetic inhibitor with anticancer activity that inhibits polymerization of microtubule protein subunits by preventing lengthening and shortening of microtubules during cell division.Eribulin is used in the study of metastatic breast cancer and solid tumors.

DC1 can be used to synthesize antibody-drug conjugates targeted to the treatment of cancer, is an ADC cytotoxin, similar to the small groove-binding DNA alkylating agent CC-1065.

Hemiasterlin is a cytotoxic peptide that acts by inducing mitotic arrest and abnormal spindle formation.

PNU-159682 carboxylic acid is a potent ADCs cytotoxin,PNU-159682 carboxylic acid has protein fold and diverse functions.

Luisol A, an aromatic tetraol and anthraquinone antibiotic analog, serves as a significant metabolite produced by an estuarine marine actinomycete from the genus Streptomyces. Additionally, it functions as an ADC (Antibody-Drug Conjugate) cytotoxin [1].

DGN462 is an effective DNA alkylating agent with anti-tumor activity, as in acute myeloid leukemia (AML). DGN462 can be used as a cytotoxic component of antibody-drug conjugates (ADCs).

Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng/ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovani, and T. b. brucei but also induces cytotoxicity in HepG2 cells (IC50s = 1.1, 72.5, 77, and 24.5 nM, respectively).

Fmoc-MMAF-OMe is a tubulin polymerization inhibitor and anticancer agent featuring an Fmoc protecting group. Its active component, MMAF, serves as the cytotoxic (ADC Cytotoxin) element in conventional antibody-drug conjugates (ADCs) [1].

γ-Amanitin, an ADC (antibody-drug conjugate) cytotoxin isolated from mushrooms, inhibits RNA polymerase II, disrupting mRNA synthesis. It exhibits effects akin to those of α-Amanitin and β-Amanitin.

Tubulysin IM-2 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins .

ε-Amanitin is a cyclic peptide obtained from various mushroom species. It exhibits a strong affinity for RNA polymerase II and effectively inhibits its activity.

Hemiasterlin Derivative-1, a derivative of hemiasterlin, is utilized in the synthesis of Antibody-Drug Conjugates (ADC).

Tomaymycin DM, a derivative of Tomaymycin, functions as a DNA alkylator and PBD dimer. It is utilized to formulate antibody-drug conjugates (ADCs) by attaching to tumor-targeting antibodies.

Rebeccamycin is an antitumor antibiotic+ inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I. It also has a negligible effect on protein kinase C and topoisomerase II.

Sulfo-DGN462 sodium undergoes degradation to DGN462 when subjected to culture medium and plasma. DGN462, a highly effective DNA-alkylating agent, exhibits anti-tumor properties that are particularly active against acute myeloid leukemia (AML).

7Ethanol-10NH2-11F-Camptothecin, an antibody drug conjugate (ADC), demonstrates inhibitory effects on tumor growth and is utilized in cancer research [1].

Tubulysin A is a natural product from myxobacterial. It has many function in vitro assays, including anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, and anti-angiogenic.

DM3 (Maytansinoid DM3) is a maytansine mimic containing disulfide or thiol groups and a tubulin inhibitor. It is the cytotoxic part of antibody-drug conjugates (ADCs) .

10NH2-11F-Camptothecin, an antibody-drug conjugate (ADC), exhibits antitumor activity and is utilized in cancer research [1].

Suicin 65, a class I type B lantibiotic synthesized by Streptococcus suis, exhibits activity against all S. suis isolates [1].

β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom, and inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis.

Fmoc-MMAE, a protective group-conjugated variant of monomethyl auristatin E (MMAE), serves as a powerful inhibitor of tubulin. It finds application in the synthesis of antibody-drug conjugates (ADC).

CC-885-CH2-PEG1-NH-CH3 is a neoDegrader compound employed for the production of Antibody neoDegrader Conjugate (AnDC) during synthesis.

Aminohexylgeldanamycin (AHGDM) hydrochloride is a Geldanamycin derivative and a powerful inhibitor of HSP90. It exhibits significant antiangiogenic and antitumor properties.

Duostatin 5 (Duo-5) is a sea hare toxin analog commonly used in the synthesis of ADC compounds.

Docetaxal, also known as 10-Acetyl docetaxel, is an analog of Docetaxel exhibiting potent anticancer properties. It acts as a microtubule disassembly inhibitor, effectively inhibiting mitosis.

Duocarmycin SA is an extremely potent cytotoxic agent and antitumor antibiotic that induces sequence-selective alkylation of duplex DNA, with an IC50 of 10 pM. It demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells when combined with proton radiation in vitro.

7-Aminomethyl-10-methyl-11-fluoro camptothecin, serving as a cytotoxic component of the antibody-drug conjugate (ADC) MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin, is employed in the synthesis of camptothecin ADCs [1].

Seco-DUBA hydrochloride is a toxin for ADC drug SYD985.

Dolastatin 15, a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the anti-tubulin agent Dolastatin 10. Dolastatin 15 can be used as an ADC cytotoxin and it induces cell cycle arrest and apoptosis in m

Tubulysin D is a tetrapeptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis, and displays potent antitumor activity.

N-Me-L-Ala-maytansinol used for making antibody-drug conjugate (ADC),is a hydrophobic, cell permeable payload.

Seco-DUBA, a duocarmycin (DUBA) prodrug, possess two hydroxyl groups suitable for antibody coupling through a linker. This compound, serving as a precursor, enables the synthesis of antibody-drug conjugates (ADCs).

Tubulysin family are originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis, and are potent microtubule destabilizing agents.