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: C15H16F5N3O5
- Molecular Weight: 413.30
N3-PEG3-C2-PFP ester is a nonclaevable 3-unit PEG linker used in the synthesis of antibody-drug conjugates (ADCs). N3-PEG3-C2-PFP 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: C13H12F5N3O4
- Molecular Weight: 369.24
N3-PEG2-C2-PFP ester is a nonclaevable 2-unit PEG linker used in the synthesis of antibody-drug conjugates (ADCs). N3-PEG2-C2-PFP 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: C9H14O6
- Molecular Weight: 218.20
6-O-2-Propyn-1-yl-D-galactose is a nonclaevable glycolinker for the functionalization of cytotoxic agents and applications in antibody-agent conjugation. 6-O-2-Propyn-1-yl-D-galactose 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: C23H24N2O6
- Molecular Weight: 424.45
(R)-Fmoc-Gly-NHCH2O-CH(cPr)-COOH (Compound A-99-1) is an ADC linker that can be used for the synthesis of ADCs.
- Formula: C26H34N6O9
- Molecular Weight: 574.58
- Formula: C16H31N5O4
- Molecular Weight: 357.45
N3-D-Orn(Boc)-OH (CHA) is a Boc-protected pentanoic amino acid derivative, can be used as a click chemistry reagent and has been used to synthesis antibody-drug conjugates (ADC). It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
- Formula: C10H18N4O4
- Molecular Weight: 258.27
N3-D-Orn(Boc)-OH is a Boc-protected pentanoic amino acid derivative, can be used as a click chemistry reagent and has been used to synthesis antibody-drug conjugates (ADC). It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
- Formula: C18H34N6O3
- Molecular Weight: 382.50
N3-L-Cit-OH DCHA is a click chemistry reagent containing an azide group. N3-L-Cit-OH DCHA can be used to construct peptidomimetic ADC linkers using Click-chemistry. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
- Formula: C6H11N5O3
- Molecular Weight: 201.18
N3-L-Cit-OH is a click chemistry reagent containing an azide group. N3-L-Cit-OH can be used to construct peptidomimetic ADC linkers using Click-chemistry. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
- Formula: C27H30N4O8
- Molecular Weight: 538.55
4-Pentynoyl-Val-Ala-PAB-PNP is a cleavable ADC linker, that has been used to synthesis cryptophycin conjugates. 4-Pentynoyl-Val-Ala-PAB-PNP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
