A cytotoxic agent used in antibody-drug conjugates

A novel potent DNA-intercalating payload dimer (PBD dimer) payload for antibody-drug conjugates (ADCs).

MMAF-Ome belongs to ADC, and inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4-) cell lines, respectively.

Maytansinol inhibits microtubule assembly and induces microtubule disassembly in vitro. Target: Microtubule/Tubulin in vitro: Maytansinol disrupts the mitotic spindle and prevents mitotic exit in Drosophila. Maytansinol reduces the growth and/or survival of HCT116 cells in a dose-dependent manner and that the effect was more severe for p53+/+ than for p53-/- cells at both low and high doses. Maytansinol inhibits the growth of HCT116 human colon cancer cells. Maytansinol induces apoptosis in imaginal discs of wild-type larvae but not p53 mutant larvae. This parallels the finding in human HCT116 cells, in which Maytansinol was more effective when p53 was present, at least at some doses. Maytansinol induces apoptosis in imaginal discs of wild-type larvae but not p53 mutant larvae at 24 hours after exposure to drug.

Ansamitocin P-3, a potent anti-tumor maytansinoid found in Actinosynnema pretiosum, is a maytansine analog which displays potent cytotoxicity against the human solid tumor cell lines A-549 and HT-29.

Calicheamicin, also known as Calicheamicin gamma(1,I) or Calichemicin gamma1, is an potent enediyne antitumor antibiotics derived from the bacterium Micromonospora echinospora. Calicheamicin targets DNA and cause strand scission. Calicheamicin binds with DNA in the minor groove, wherein it then undergos a reaction analogous to the Bergman cyclization to generate a diradical species. This diradical, 1,4-didehydrobenzene, then abstracts hydrogen atoms from the deoxyribose (sugar) backbone of DNA, which ultimately leads to strand scission. The specificity of binding of calicheamicin to the minor groove of DNA is due to the aryltetrasaccharide group of the molecule.

Daun02 is a daunorubicin b-galactoside prodrug for use in conjunction.

Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM.

OSW-1 is a natural anti-enterovirus and anti-cancer compound that targets oxysterol-binding protein (OSBP) with Ki of 26 and 54 nM for OSBP and ORP4L, respectively.

PNU-159682 is a major bioactive metabolite of Nemorubicin in human liver microsomes; > 3,000-fold cytotoxic than its parent compound(MMDX and doxorubicin).

SG3199 is a PBD dimer warhead component of antibody-drug conjugate (ADC) payload tesirine, demonstrates potently cytotoxic against a panel of human solid tumour and haematological cancer cell lines with mean GI50 of 151.5 pM.

SGD-1882 (PBD dimer, Pyrrolobenzodiazepine dimer) is a novel potent DNA-intercalating payload dimer (PBD dimer) payload for antibody-drug conjugates (ADCs)..

Monomethyl auristatin E (MMAE; Vedotin) is a hot topic in Antibody-drug conjugates (ADCs) studies. It is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin.

Maytansine, a benzoansamacrolide, is a highly potent microtubule-targeted compound that induces mitotic arrest and kills tumor cells at subnanomolar concentrations. However, it failed as an anticancer agent in human clinical trials because of lack of tumo

Dimethyl-SGD-1882 (Dimethyl-PBD dimer) is a highly potent DNA alkylator, and is used as an antibody-drug conjugate (ADC) cytotoxin. PBD Dimer is a DNA alkylator which inhibits DNA replication.

DC10SMe is a DNA alkylator, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC10SMe exhibits IC50s of 15 pM, 12 pM, and 12 pM for Ramos, Namalwa, and HL60/s cancer cells, respectively.

DC4SMe, a phosphate prodrug of cytotoxic DNA alkylator DC4, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4SMe exhibits IC50s of 1.9 nM, 2.9 nM, and 1.8 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC4SMe can be used for the targeted treatment of cancer.

DC44SMe, a phosphate prodrug of cytotoxic DNA alkylator DC44, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC44SMe exhibits IC50s of 2.0 nM, 2.8 nM, and 1.9 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC44SMe can be used for the targeted treatment of cancer.

DC4, a ADC cytotoxin, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4 can be used for the targeted treatment of cancer.

DC44, a ADC cytotoxin, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC44 can be used for the targeted treatment of cancer.

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 a

Maytansinoid DM4, a chemical derivative of maytansine, is a potent and selective cytotoxic agent with promising anticancer properties. Anticancer properties of maytansinoids have been attributed to their ability to disrupt microtubule function. Maytansin