ADC Synthesis
Click chemistry has been increasingly used by bioinorganic and medicinal chemists in the study of targeted medicines, such as antibody-drug conjugates (ADCs). ADC is mainly composed of three parts: antibody, payload, and linker. A variety of click chemistry methodologies have been used to attach payloads to antibodies. One advantage of click chemistry is that the reaction is very efficient and high-yielding, and occurs under mild conditions. Several other companies are using “Click chemistry” to create ADCs, some of which have entered clinical trials, such as ADCT-601 and STRO-002. ADC activation with “click-to-release” chemistry on a tumor cell is reported, it demonstrates high tumor uptake of the ADC, its direct chemically controlled activation and good tumor retention of the released model drug, laying the foundation for future therapy research.
- Formula: C7H13NO2
- Molecular Weight: 143.18
Propargyl-PEG2-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG2-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG2-amine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
- Formula: C7H8N4O4
- Molecular Weight: 212.16
N3-C2-NHS ester is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N3-C2-NHS ester is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
- Formula: C24H33N3O7
- Molecular Weight: 475.53
BCN-endo-PEG2-maleimide is an ADC Linker containing 4 PEG units. BCN-endo-PEG2-maleimide contains the lyophilic bidentate macrocyclic ligand endo-BCN, which can further synthesize macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.
- Formula: C46H49N7O10
- Molecular Weight: 859.92
DBCO-Val-Cit-PABC-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-Val-Cit-PABC-PNP is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
- Formula: C27H48N8O7S3
- Molecular Weight: 692.91
Biotin-PEG3-SS-azide is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Biotin-PEG3-SS-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
- Formula: C67H106N10O16
- Molecular Weight: 1307.62
Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) consists the ADCs linker (Acetylene-linker-Val-Cit-PABC) and potent tubulin inhibitor (MMAE). Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) is a agent-linker conjugate for ADC. Acetylene-linker-Val-Cit-PABC-MMAE is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
- Formula: C34H47N9O12
- Molecular Weight: 773.79
Azido-PEG3-Val-Cit-PAB-PNP is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG3-Val-Cit-PAB-PNP is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG3-Val-Cit-PAB-PNP is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
- Formula: C26H38N2O10
- Molecular Weight: 538.59
BCN-endo-PEG4-NHS is an ADC Linker containing 4 PEG units. BCN-endo-PEG4-NHS contains the lyophilic bidentate macrocyclic ligand endo-BCN, which allows for further synthesis of macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
- Formula: C29H46N4O7S
- Molecular Weight: 594.76
BCN-PEG3-Biotin is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). BCN-PEG3-Biotin is a click chemistry reagent, it contains a BCN group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
- Formula: C8H10N4O4
- Molecular Weight: 226.19
N3-C3-NHS ester is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N3-C3-NHS ester is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
- Formula: C12H23N9O2
- Molecular Weight: 325.37
bisSP1 is an antibody-drug conjugate linker (ADC Linkers). bisSP1 is also a click chemistry reagent that undergoes copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Alkyne groups, and strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
- Formula: C19H23N7O2S
- Molecular Weight: 413.50
Tetrazine-biotin is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Tetrazine-biotin is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.
- Formula: C22H35NO8
- Molecular Weight: 441.52
endo-BCN-PEG4-acid is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). endo-BCN-PEG4-acid is a click chemistry reagent, it contains a BCN group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
- Formula: C35H55N9O12S
- Molecular Weight: 825.93
PC Biotin-PEG3-azide is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). PC Biotin-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
- Formula: C48H50N4O8
- Molecular Weight: 810.93
DBCO-PEG4-DBCO is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. DBCO-PEG4-DBCO is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG4-DBCO is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
- Formula: C29H36N4O7
- Molecular Weight: 552.62
DBCO-PEG3-oxyamine is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG3-oxyamine is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
- Formula: C28H27N3O6S2
- Molecular Weight: 565.66
DBCO-CONH-S-S-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-CONH-S-S-NHS ester is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
- Formula: C15H24N4O7S2
- Molecular Weight: 436.50
Azido-PEG3-SS-NHS is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG3-SS-NHS is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
- Formula: C19H32N4O10
- Molecular Weight: 476.48
Azido-PEG6-NHS ester is a cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG6-NHS ester is also a PEG- and Alkyl/ether based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG6-NHS ester is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
- Formula: C8H18N4O4
- Molecular Weight: 234.25
Aminooxy-PEG3-azide is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Aminooxy-C2-PEG3-azide is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Aminooxy-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
