NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
sulfo-SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4) via the sulfo-SPDB linker.
Mal-PEG2-VCP-Eribulin consists the ADCs linker (Mal-PEG2-VCP) and Eribulin[1]. Eribulin is a mechanistically unique microtubule inhibitor for cancer[2]. Mal-PEG2-VCP-Eribulin is an Eribulin-based drug for antibody conjugates[1].
MC-Sq-Cit-PAB-Gefitinib has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Sq-Cit-PAB-Gefitinib is used for the antibody-drug conjugates (ADC) to treat various diseases or disorders, e.g. characterized by the overexpression of a tumor antigen[1,2].
mDPR-Val-Cit-PAB-MMAE consists the ADCs linker (mDPR-Val-Cit-PAB) and potent tubulin inhibitor (MMAE), mDPR-Val-Cit-PAB-MMAE is an antibody drug conjugate.
VCP-Eribulin consists the ADCs linker (VCP) and Eribulin[1]. Eribulin is a mechanistically unique microtubule inhibitor for cancer[2]. VCP-Eribulin is an Eribulin-based drug for antibody conjugates[1].
MC-Val-Cit-PAB-rifabutin has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-rifabutin is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate (ADC).
Mertansine (DM1) is a microtubulin inhibitor which binds at the tips of microtubules and suppresses the dynamicity of microtubules.. Mertansine is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.
MC-Val-Cit-PAB-vinblastine has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-vinblastine is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
MC-Sq-Cit-PAB-Dolastatin10 has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Sq-Cit-PAB-Dolastatin10 is used for the antibody-drug conjugates (ADC) to treat various diseases or disorders, e.g. characterized by the overexpression of a tumor antigen[1,2].
SMCC-DM1 is DM1 with a reactive linker SMCC to make antibody drug conjugate. DM1 (mertansine), a thiol-containing maytansinoid, is a potent microtubule-disrupting agent.
C-11 is a tubulysin-based antibody–drug conjugates (ADCs), displays cytotoxicity for carcinoma cell lines[1].
pH-susceptible lactone (Drug linker 1) is a pH-susceptible lactone-linked SN-38 drug linker. pH-susceptible lactone is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively[1].
Nitro-PDS-Tubulysin M has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. Nitro-PDS-Tubulysin M is used for the antibody-drug conjugates (ADC) to treat various diseases or disorders, e.g. characterized by the overexpression of a tumor antigen[1,2].
AmPEG6C2-Aur0131 is a non-cleavable anti-CXCR4 drug-linker conjugates for ADC.
MC-Val-Cit-PAB-tubulysin5a has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-tubulysin5a is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulin inhibitor (MMAD), Vc-MMAD is an antibody drug conjugate.IC50 Valu: N/ATarget: tubulin; ADCsMonomethyl auristatin D (MMAD), a potent tubulin inhibitor, is a toxin payload and antibody drug conjugate.For comparison purposes, the ADC A1 -mc-MMAD and/or A1 -vc-MMAD were used. The linker payload, mc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) was conjugated to the A1 anti-5T4 monoclonal antibody through a cysteine residue at a ratio of approximately 4 drug moieties per antibody molecule. The linker payload mc- Val-Cit-PABA-MMAD or vc-MMAD (maleimidocapronic -valine-citruline-p- aminobenzyloxycarbonyl- monomethylauristatin-D) was conjugated to the A1 anti-5T4 monoclonal antibody through a cysteine residue at a ratio of approximately 4 drug moieties per antibody molecule (Antibody-drug conjugates Patent: WO 2013068874 A1).
MC-Val-Cit-PAB-clindamycin has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-clindamycin is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
MC-Val-Cit-PAB-retapamulin has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-retapamulin is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate; Mc-MMAD is a protective group (maleimidocaproyl) -conjugated MMAD.IC50 Value:Target: tubulin; ADCsFor comparison purposes, the ADC A1 -mc-MMAD and/or A1 -vc-MMAD were used. The linker payload, mc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) was conjugated to the A1 anti-5T4 monoclonal antibody through a cysteine residue at a ratio of approximately 4 drug moieties per antibody molecule. The linker payload mc- Val-Cit-PABA-MMAD or vc-MMAD (maleimidocapronic -valine-citruline-p- aminobenzyloxycarbonyl- monomethylauristatin-D) was conjugated to the A1 anti-5T4 monoclonal antibody through a cysteine residue at a ratio of approximately 4 drug moieties per antibody molecule (Antibody-drug conjugates Patent: WO 2013068874 A1).
Acetylene-linker-Val-Cit-PABC-MMAE consists the ADCs linker (Acetylene-linker-Val-Cit-PABC) and potent tubulin inhibitor (MMAE), Acetylene-linker-Val-Cit-PABC-MMAE is an antibody drug conjugate.
MC-Val-Cit-PAB-indibulin has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-indibulin is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
MC-VC-PABC-DNA31 has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-VC-PABC-DNA31 is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
MC-Val-Cit-PAB-carfilzomib has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-carfilzomib is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4) via a SPDB linker, exhibiting potent anti-tumor activity.
AcLys-PABC-VC-Aur0101 is a cleavable anti-CXCR4 drug-linker conjugates for ADC.
MC-Val-Cit-PAB-duocarmycin has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-duocarmycin is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
VcMMAE is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
Deruxtecan analog is a drug-linker conjugate for antibody-drug conjugate (ADC) extracted from patent WO2017002776A1, compound 1.