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

CL2A-SN38 is a SN38 derivative with a peptide-linker which can easily react with antibody to form an antibody-drug conjugate (ADC). CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate

DC41 is a DC1 derivative. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer.

Luisol A, an aromatic tetraol, is a major metabolite of an estuarine marine actinomycete of the genus Streptomyces. Luisol A, anthraquinone antibiotic analog, is an ADC Cytotoxin.

Boc-NMe-Val-Val-Dil-Dap-OH is an ADC Cytotoxin.

Boc-Val-Dil-Dap-OH is an ADC Cytotoxin.

Boc-Val-Dil-Dap-Phe-Ome is an ADC Cytotoxin.

Diacetyl Agrochelin is an acetyl derivative of Agrochelin, which is produced by the fermentation of a marine Agrobacterium sp. Diacetyl Agrochelin has cytotoxic activity in tumor cell lines.

Puwainaphycin F, a cyanobacterial cyclic lipopeptide, is a moderate cytotoxin isolated from the soil cyanobacterium Cylindrospermum alatosporum C24/89. Puwainaphycin F causes necrotic cell death to mammalian cells via cell membrane permeabilization and subsequent unusual actin relocalization.

Mytoxin B is an ADC cytotoxin. Mytoxin B is a satratoxin-type trichothecene macrolide and is similar to the effect of LY294002. Mytoxin B induces cell apoptosis via PI3K/Akt pathway.

Muscotoxin A is an?ADC cytotoxin. Muscotoxin A is a cytotoxic lipopeptide that permeabilizes mammalian cell membranes and induces necrotic cell death.

Sandramycin ia a cyclic depsipeptide antibiotic isolated from cultured broth of a Nocardioides sp. Sandramycin is also a DNA intercalator that potently binds DNA and is an ADC cytotoxin. Sandramycin is active against Gram-positive bacteria and has potent antitumor activity.

CL2-SN-38 is a cleavable linker-based antibody-drug conjugate (ADC) containing the topoisomerase I inhibitor SN-38 and a maleimidocaproyl linker. CL2-SN-38 has been linked to tumor-selective human monoclonal antibodies, such as anti-CEACAM5 (hMN-14) to target SN-38 to tumor sites and improve its solubility. CL2-SN-38 linked to hMN-14 binds (Kd = 1.4 nM) and is cytotoxic to LoVo human colon adenocarcinoma cells (IC50 = 5.3 nM). CL2-SN-38 linked to hMN-14 increases survival in a colon carcinoma mouse model of lung metastasis.

Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer.

7-Aminomethyl-10-methyl-11-fluoro camptothecin is a cytotoxin of MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin. 7-Aminomethyl-10-methyl-11-fluoro camptothecin can be used for the synthesis of camptothecin antibody-drug conjugate (ADC).

MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin (compound 21a), a camptothecin payload, can be conjugated to a monoclonal antibody (mAb) for the synthesis of camptothecin antibody-drug conjugate (ADC).

7-MAD-MDCPT, a Camptothecin analog, is a toxin payload in antibody drug conjugates (ADCs).

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

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC.

N-​Me-​L-​Ala-​maytansinol is a maytansine derivative. .N-​Me-​L-​Ala-​maytansinol can be used for synthesis of antibody-drug conjugate (ADC).

Tubulysin IM-1 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins.

Azonafide-PEABA is a cytotoxic drug moiety.

DMEA-PNU-159682 (molecule D12) is a ADC cytotoxin molecule including metabolites of nemorubicin (MMDX) from liver microsomes and a potent ADCs cytotoxin PNU-159682.

Seco-DUBA is a duocarmycin (DUBA) prodrug containing two hydroxyl groups, which can each be used for coupling to an antibody via a linker. Seco-DUBA can be used in the synthesis of antibody-drug conjugates (ADCs).

Corixetan is a highly efficient thorium chelator. Corixetan can efficiently complex Th-227 with sufficient in vivo stability.

CC-885-CH2-PEG1-NH-CH3 is a neoDegrader that can be used in the synthesis of Antibody neoDegrader Conjugate (AnDC).

Duostatin 5 is a potent mitotic inhibitor by inhibiting tubulin polymerization.

SC209, an ADC cytotoxin extracted from patent WO2021247798, is used in synthesis of anti-EGFR antibody-drug conjugate ADC.

Deruxtecan, a topoisomerase I inhibitor, is an exatecan derivative (DX-8951 derivative) with a cleavable pepetide linker and a maleimide group. The maleimide group in Deruxtecan can react with antibody to form antibody-drug conguates (ADC) such as Trastuzumab deruxtecan (DS-8201a), which is a HER2-targeting antibody–drug conjugate.

Tomaymycin DM, a DNA alkylator, is a derivative of Tomaymycin, it is a PBD dimer, which is attached to tumor targeting antibodies to create antibody-drug conjugates (ADCs).

Gly-Cyclopropane-Exatecan involves in the synthesis of anti-B7-H4 ADC, containing Exatecan, a DNA Topoisomerase I inhibitor. Gly-Cyclopropane-Exatecan participated in the formation of the ADC hu2F7-Exatecan (compound 34), which showed antitumor activity in vivo and in vitro.

Dox-btn2 is a biotinylated derivative of Doxorubicin, with a biotin label at the point of conjugation to doxorubicin at 3'-NH2. Dox-btn2 can be used for cell imaging. While Doxorubicin is mainly accumulated in the nucleus, while Dox-btn2 is mainly located in the cytoplasm.