adc payload

Duocarmycin TM is a DNA alkylator. Duocarmycin TM is an exceptionally potent antitumor antibiotic.

Dxd (OQM5SD32BQ) is a potent inhibitor of DNA topoisomerase I with an IC50 of 0.31 μM. It is used as a conjugated drug of HER2-targeting ADC.

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.

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

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.

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

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

Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor

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

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

PC Mal-NHS carbonate ester is a cleavable linker specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. This chemical compound facilitates drug-antibody conjugation, enabling targeted delivery and enhanced therapeutic efficacy. Its unique carbonate ester structure allows efficient cleavage in the targeted environment, ensuring controlled drug payload release, highlighting its significance in innovative and targeted cancer therapies.

NAMPT inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). It contains the microtubule polymerization inhibitor DM1 as the active metabolite, which inhibits microtubule polymerization. It is commonly used in breast cancer research.

Nampt-IN-10 trihydrochloride (Compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor exhibiting cellular potency against A2780 and CORL23 cell lines, with IC50 values of 5 nM and 19 nM, respectively. It holds potential as a novel non-antimitotic payload for antibody-drug conjugate (ADC) [1].

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

SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) applications, employing the maytansine-based payload DM4 (a tubulin inhibitor) connected through a SPDB linker. This compound demonstrates significant anti-tumor efficacy.

m-PEG4-Br is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADC) for Trastuzumab, positioned distally from the monomethyl auristatin E (MMAE) payload to produce an ADC with modified hydrophilicity, antigen binding, and in vitro potency[1].