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: C23H18N2O5
- Molecular Weight: 402.40
DBCO-NHS ester is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-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: C18H16N2O
- Molecular Weight: 276.34
DBCO-amine is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups. DBCO-amine is used in the synthesis of antibody-drug conjugates (ADCs).
- Formula: C88H128N12O19
- Molecular Weight: 1658.03
DBCO-PEG4-VC-PAB-MMAE consists a ADC linker (DBCO-PEG4-VC-PAB) and a tubulin polymerization inhibitor MMAE (HY-15162). DBCO-PEG4-VC-PAB-MMAE can be used in the synthesis of antibody-agent conjugates (ADCs). MMAE is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. DBCO-PEG4-VC-PAB-MMAE 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: C19H15NO3
- Molecular Weight: 305.33
DBCO-acid is a click chemistry reagent used in the synthesis of ADC linker DBCO-NHS ester ((HY-115524) and (HY-115545)), and agent-linker conjugates DBCO-PEG-MMAE (HY-111012 and HY-126690). DBCO-acid contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
- Formula: C72H79FN10O17
- Molecular Weight: 1375.45
DBCO-PEG4-GGFG-Dxd is a agent-linker conjugate for ADC with potent antitumor activity by using Dxd (a DNA topoisomerase I inhibitor), linked via the cleavable ADC linker DBCO-PEG4-GGFG. DBCO-PEG4-GGFG-Dxd 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: C108H128F2N20O31S2
- Molecular Weight: 2304.41
- Formula: C61H75FN8O15
- Molecular Weight: 1179.29
W1507 is an NH2-TML-based linker-payload conjugate, in which the payload is Exatecan (HY-13631) and the linker is Mal-PEG4-Val-Ala-Ph-2,2-dimethylpropanoic acid (HY-184906). W1507 can be conjugated with Trastuzumab (HY-P9907) to synthesize the ADC Her2-W1507. Her2-W1507 exhibits in vivo anti-tumor activity. W1507 can be used for the research of gastric cancer, ovarian adenocarcinoma and Her2-amplified breast cancer.
- Formula: C67H82FN13O19
- Molecular Weight: 1392.44
- Formula: C6H14N4O2
- Molecular Weight: 174.20
Azido-PEG2-C2-amine (N3-PEG2-CH2CH2NH2) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG2-C2-amine is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG2-C2-amine 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: C15H24N4O8
- Molecular Weight: 388.37
N3-PEG4-C2-NHS ester is a nonclaevable 4-unit PEG linker used in the synthesis of antibody-drug conjugates (ADCs). N3-PEG4-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: C36H42N4O9
- Molecular Weight: 674.74
DBCO-PEG4-Maleimide is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG4-Maleimide 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: C6H14N4
- Molecular Weight: 142.20
6-Azido-hexylamine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 6-Azido-hexylamine 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: C25H22N2O5
- Molecular Weight: 430.45
DBCO-NHS ester 2 is a cleavable linker that is used for making antibody-drug conjugate (ADC). DBCO-NHS ester 2 is a derivative of Dibenzylcyclooctyne (DBCO) used in copper-free click chemistry[1]. DBCO-NHS ester 2 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: C35H46N6O9
- Molecular Weight: 694.77
Gly-Gly-Gly-PEG4-DBCO is a 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Gly-Gly-Gly-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: C25H21N3O4
- Molecular Weight: 427.45
DBCO-Maleimide is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-Maleimide 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: C88H126N12O20
- Molecular Weight: 1672.01
DBCO-PEG4-Val-Cit-PAB-MMAF consists a cleavable 4 unit PEG ADC linker (DBCO-PEG4-Val-Cit-PAB) and a potent tubulin polymerization inhibitor (MMAF). DBCO-PEG4-Val-Cit-PAB-MMAF can be used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG4-Val-Cit-PAB-MMAF 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: C36H43N3O11
- Molecular Weight: 693.74
DBCO-PEG5-NHS ester is a PEG/Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs. DBCO-PEG5-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG5-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: C6H12BrN3O2
- Molecular Weight: 238.08
Bromo-PEG2-C2-azide is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Bromo-PEG2-C2-azide is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Bromo-PEG2-C2-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: C11H21N3O6
- Molecular Weight: 291.30
Azido-PEG4-C2-acid a PEG-based PROTAC linker can be used in the synthesis of vRucaparib-TP4. Azido-PEG4-C2-acid is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG4-C2-acid 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: C23H40N4O12
- Molecular Weight: 564.58
Azido-PEG8-NHS ester is a cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG8-NHS ester is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG8-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.
