adc payload

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.

Doxorubicin (Adriamycin) is a fluorescent anthracycline antitumor antibiotic that inhibits Topoisomerase I/II, induces apoptosis and autophagy, downregulates the AMPK signaling pathway, and is commonly used in cancer chemotherapy as well as in models of nephritis and heart failure.

Maytansinol (Ansamitocin P-0) inhibits microtubule assembly and causes microtubule disassembly in vitro.

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

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.

SN-38 (NK012) is the active metabolite of Irinotecan, a DNA topoisomerase I (Topo I) inhibitor, which inhibits DNA and RNA synthesis (IC50=0.077/1.3 μM). SN-38 has antitumor activity and induces autophagy.

Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor

Auristatin E, a cytotoxic tubulin modifier, disrupts cell division by inhibiting tubulin polymerisation. This compound demonstrates potent and selective antitumor activities, serving as an MMAE analog and cytotoxin in antibody-drug conjugates.

Duocarmycin TM belongs to natural products, serving as a DNA alkylating agent with sequence-selective double-stranded DNA alkylation capability, featuring high cell permeability and potent antitumor activity, for targeted therapy including drug-resistant and low-proliferative tumors.

Dxd (OQM5SD32BQ) is a potent DNA topoisomerase I inhibitor (IC50= 0.31 μM). Dxd was used as a conjugate drug for HER2-targeted ADCs.

MMAF-OMe (Monomethyl auristatin F methyl ester) is an antitubulin agent which 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. MMAF-Ome is also an ADC cytotoxin.

Auristatin F is an effective inhibitor of microtubule and vascular damaging agent. Auristatin F can be used in antibody-drug conjugates.

DM4 (Ravtansine) can be used in the preparation of antibody drug conjugate and it is an antitubulin agent. It can inhibit cell division.

PNU-159682, a metabolite of anthracycline nemorubicin, is a DNA topoisomerase II inhibitor with excellent cytotoxicity.

Ansamitocin P 3' (Maytansinol butyrate) is an antibody-drug conjugate cytotoxin with antitumor activity.

DM1-SMe (DM1-SSMe) is a potent inhibitor of maytansinoid microtubular. DM1-SMe is about 3 to 10-fold more potent than the parent drug Maytansine, with IC50s of 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines.

MMAF (MonoMethyl auristatin F), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin.

MMAD (Demethyldolastatin 10) is a potent tubulin inhibitor. MMAD is a toxin payload in antibody drug conjugates (ADCs).

10-Deacetyl-7-xylosyl paclitaxel (7-Xylosyl-10-deacetyltaxol) is a Paclitaxel derivative with improved pharmacological features and higher water solubility,used in Chinese clinics to treat cancer.

Monomethyl auristatin E (MMAE) (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity.

Dolastatin 10 (DLS 10) is a potent peptide with antimitotic properties, effectively inhibiting tubulin polymerization.

ABBV-969 Payload (Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT) is a drug-linker conjugate employed in the synthesis of antibody-drug conjugates (ADCs). The ABBV-969 Payload contains a Topoisomerase I inhibitor molecule and a chemical linker, enabling coupling with anti-c-Met antibodies to generate ABBV-969 ADCs with targeted anticancer activity.

Rinatabart sesutecan is a highly homogeneous antibody-drug conjugate (ADC) targeting folate receptor alpha (FRα). Rinatabart sesutecan consists of a humanized antibody targeting FRα, a hydrophilic cleavable linker, and the topoisomerase I inhibitor exatecan as the payload. It is primarily used for the targeted treatment and mechanistic research of folate receptor-positive solid tumors.

Sacituzumab tirumotecan (SKB264) is an antibody-drug conjugate (ADC) targeting TROP2 (trophoblast cell surface antigen 2), capable of releasing the active payload KL610023 within TROP2-positive tumour cells. an effective topoisomerase I inhibitor that induces DNA damage and leads to cell cycle arrest and apoptosis, for use in non-small cell lung cancer (NSCLC) and triple-negative breast cancer (TNBC).