Antibody-drug Conjugates (ADC)

Fmoc-NH-PEG6-alcohol is a cleavable linker specifically designed for the synthesis of antibody-drug conjugates (ADCs). This reagent plays a crucial role in enhancing the efficacy and specificity of ADCs by facilitating the controlled release of cytotoxic agents upon internalization. Its structure promotes solubility and stability, making it suitable for various research applications, including cancer therapeutics and targeted drug delivery studies.

P5(PEG24)-OSu is a polyethylene glycol (PEG) linker designed for antibody-drug conjugate (ADC) applications. This reagent facilitates the synthesis of PROTAC molecules, promoting targeted protein degradation. Its PEGylated structure enhances solubility and improves pharmacokinetic properties, making it a valuable tool in therapeutic research and development focused on precision medicine.

Tr-PEG4-OH is a non-cleavable four-unit polyethylene glycol (PEG) linker designed for use in antibody-drug conjugates (ADCs). Its stable structure facilitates the conjugation of cytotoxic agents to antibodies, enhancing the therapeutic efficacy while minimizing off-target effects. This linker is ideal for research applications involving ADC development and optimization for targeted cancer therapies.

Fmoc-Val-Cit-PAB is a cleavable linker for antibody-drug-conjugation (ADC).

2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) is a macrocycle DOTA derivative for tumor pretargeting.

Ozogamicin is an antibody-drug conjugate Linker.

PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).

Mc-Val-Cit-PAB-Cl is a cleavable ADC linker. Mc-Val-Cit-PAB-Cl can be used to conjugate MMAE and antibody to form antibody-MC-vc-MMAE .

Daunorubicinol is a drug-linker conjugate for ADC with potent antitumor activity by using Aur0101 (DNA Topoisomerase II inhibitor), linked via the ADC linker.

Vc-seco-DUBA is a drug-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco.

MC-VC-PABC-Aur0101 is a drug-linker conjugate for ADC with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the ADC linker MC-VC-PABC.

Fmoc-Val-Cit-PAB-PNP is a cleavable peptide linker, is a linker for antibody-drug-conjugation (ADC).

Monomethyl auristatin F (MMAF) is a synthetic antineoplastic agent. It is part of some experimental anti-cancer antibody-drug conjugates such as vorsetuzumab mafodotin and SGN-CD19A.

alpha-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.

VcMMAE is an antibody-drug conjugate (ADC) with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).

Biotin-PEG3-amineis PEG derivative containing a biotin group and a terminal primary amine group.

PSMA-617, also know as vipivotide tetraxetan. It is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer.

CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1/2 ~20 hours).

CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types.

L2A is a claevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. Labetuzumab govitecan used this linker.

EC089 is a cleavable linker used in conjugates of tubulysins and folates, and extracted from patent WO2011069116A1.

EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC).

6-O-2-Propyn-1-yl-D-galactose is a nonclaevable glycolinker for the functionalization of cytotoxic drugs and applications in antibody-drug conjugation.

Fmoc-PEA (Example 1-2) is a used as a cleavable linker for antibody-drug conjugates (ADC).

SPP is a cleavable disulfide linker, can be used to form cytotoxic compound- linker conjugate.

AMAS is a nonclaevable heterobifunctional crosslinker with NHS ester and maleimide groups that allows covalent conjugation of amine- and sulfhydryl-containing molecules.

Duocarmycin is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity. Duocarmycin is a DNA minor groove binding alkylating agent and explored as drug?Cantibody conjugates (ADCs) .

MC-Val-Cit-PAB-tubulysin5a is a drug-linker conjugate for ADC with potent antitumor activity by using tubulysin5a (a tubulin inhibitor), linked via the ADC linker MC-Val-Cit-PAB.

MC-Val-Cit-PAB-rifabutin is a drug-linker conjugate for ADC with potent antitumor activity by using rifabutin (an DNA-dependent RNA polymerase inhibitor), linked via the ADC linker MC-Val-Cit-PAB.

MC-Val-Cit-PAB-Indibulin is a drug-linker conjugate for ADC with potent antitumor activity by using Indibulin (an orally applicable inhibitor of tubulin assembly), linked via the ADC linker MC-Val-Cit-PAB.

MC-Val-Cit-PAB-clindamycin is a drug-linker conjugate for ADC with potent antitumor activity by using clindamycin (a protein synthesis inhibitor), linked via the ADC linker MC-Val-Cit-PAB.

MC-Val-Cit-PAB-Retapamulin is a drug-linker conjugate for ADC with potent antitumor activity by using Retapamulin (a ribosome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.

MC-Val-Cit-PAB-dimethylDNA31 is a drug-linker conjugate for ADC with potent antitumor activity by using dimethylDNA31, linked via the ADC linker MC-Val-Cit-PAB.

MC-Val-Cit-PAB-duocarmycin is a drug-linker conjugate for ADC with potent antitumor activity by using duocarmycin (a DNA minor groove binding alkylating agent), linked via the ADC linker MC-Val-Cit-PAB.

MC-Val-Cit-PAB-carfilzomib is a drug-linker conjugate for ADC with potent antitumor activity by using carfilzomib (an irreversible proteasome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.

Mc-Val-Cit-PABC-PNP is a cathepsin cleavable ADC peptide linker.

Dxd (Exatecan derivative for ADC) 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).

Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.

Val-cit-PAB-OH is a cleavable ADC linker.

PNU-159682, a highly potent metabolite of the anthracycline nemorubicin (DNA topoisomerase II inhibitor) with outstanding cytotoxicity, is a potent ADCs cytotoxin.

FBN33428, also known as Fmoc-Phe-?Lys(Boc)-PAB; is a Hydrolyzable linker for making ADC conjugate

Val-Lys(Boc)-PAB is a ADC linker.

MC-Gly-Gly-Phe is a cleavable linker used for antibody-drug conjugates (ADC).

Boc-Gly-Gly-Phe-Gly-OH is a protease cleavable linker used for the antibody-drug conjugate (ADC).

Boc-Dap-NE is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Succinic anhydride is a cyclic anhydride and a nonclaevable ADC linker extracted from patent WO2009064913A1. Succinic anhydride can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide.

MMAF-Ome, an antitubulin agent, belongs to ADC.

Mal-amido-PEG8-C2-acid (example 142) is a nonclaevable ADC linker, extracted from patent US2018339985.

sulfo-SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4, an antitubulin agent) via the sulfo-SPDB linker.

MC-Val-Cit-PAB is a cathepsin cleavable ADC linker that is used for making antibody-drug conjugate. FDA approved drugs such as brentuximab vedotin use this linker.