ADC Cytotoxin

Seco-Duocarmycin TM is a DNA alkylator agent belonging to Duocarmycins family that inhibits DNA synthesis. Seco-Duocarmycin TM is a cytotoxic agent, used as the cytotoxic component in antibody-drug conjugates (ADC).

DM3-SMe is a maytansine derivative and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM3-SMe shows highly cytotoxic activity in vitro with an IC50 of 0.0011 nM.

MMAF sodium (Monomethylauristatin F sodium) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF sodium (Monomethylauristatin F sodium) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A.

DM4-SMe is a metabolite of antibody-maytansin conjugates (AMCs) and a tubulin inhibitor, and also a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM4-SMe inhibits KB cells with an IC50 of 0.026 nM.

DC0-NH2 is an effector moiety for ADC and a simplified analog of DC1 with better stability. DC0-NH2 is about 1000-fold more cytotoxic than commonly used anticancer drugs (ex. Doxorubicin). DC0-NH2 can bind to the minor groove of DNA, followed by alkylation of adenine residues by its propabenzindole (CBI) component.

Cyclooctyne-O-PFP ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.

Hygrolidin is a macrocyclic lactone originally isolated from S.

Rebeccamycin is an indolocarbazole antibiotic produced by S.

A bacterial metabolite with anticancer activity

DM3 (Maytansinoid DM3) is a maytansine analog bearing disulfide or thiol groups and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs).

(S)-Seco-Duocarmycin SA is a DNA alkylator, cytotoxic to cancer cells, and acts as a ADC cytotoxin for antibody-drug conjugates.

Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.

PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker.

Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.

Aminohexylgeldanamycin (AHGDM), a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin shows antiangiogenic and antitumor activities.

Dxd-d5 (Exatecan-d5 derivative for ADC) is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .

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.

SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PBD) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249).

Seco-DUBA is a duocarmycin (DUBA) prodrug containing two hydroxyl groups, which can each be used for coupling to an antibody via a linker.

SGD-1882 is a cytotoxic, DNA minor-groove crosslinking agent pyrrolobenzodiazepine (PBD) dimer, acting as the payload for ADCs.

D8-MMAD is a deuterated form of MMAD, which is a microtubule disrupting agent.

PNU-159682 carboxylic acid (compound 53) is a potent ADCs cytotoxin and encodes a member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily. PNU-159682 carboxylic acid has protein fold and diverse functions, such as cell adhesion, cell-cell signalling, glycoprotein turnover, and roles in inflammation and immune response.

Duostatin 5 is a cytotoxin based on sea hare toxin design, which can be used as an effective cytotoxin in ADCs. It has advantages such as fewer synthetic steps, simple operation, less difficulty in quality control, and more stable chemical synthesis process.