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: C69H99N7O15
- Molecular Weight: 1266.56
DBCO-PEG4-MMAF is a agent-linker conjugate for ADC with potent antitumor activity by using the tubulin polymerization inhibitor, MMAF, linked via the linker DBCO-PEG4. DBCO-PEG4-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: C9H17N3O5
- Molecular Weight: 247.25
N3-PEG3-CH2CH2COOH a PEG-based PROTAC linker can be used in the synthesis of BI-3663 (HY-111546), BI-4216 and BI-0319. Azido-PEG3-acid is also a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N3-PEG3-CH2CH2COOH 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: C16H31N7O7
- Molecular Weight: 433.46
Gly-Gly-Gly-PEG4-azide is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Gly-Gly-Gly-PEG4-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: C80H127N11O19
- Molecular Weight: 1546.93
endo-BCN-PEG4-Val-Cit-PAB-MMAE is a cleavable ADC linker conjugated with drug containing 4-unit PEG, which can be used for synthesizing antibody-drug conjugates (ADCs). endo-BCN-PEG4-Val-Cit-PAB-MMAE 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: C67H109N13O16
- Molecular Weight: 1352.66
N3-PEG3-vc-PAB-MMAE is a synthesized agent-linker conjugate for ADC that incorporates the MMAE (a tubulin inhibitor ) and 3-unit PEG linker. N3-PEG3-vc-PAB-MMAE shows potent antitumor activity. N3-PEG3-vc-PAB-MMAE 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: C11H16N4O6
- Molecular Weight: 300.27
N3-PEG2-C2-NHS ester is a nonclaevable 2-unit PEG linker used in the synthesis of antibody-drug conjugates (ADCs). N3-PEG2-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: C78H127N11O19
- Molecular Weight: 1522.91
TCO-PEG4-VC-PAB-MMAE is a agent-linker conjugate for ADC. TCO-PEG4-VC-PAB-MMAE contains a cleavable ADC linker (TCO-PEG4-VC-PA) and a potent tubulin inhibitor MMAE (HY-15162). TCO-PEG4-VC-PAB-MMAE is a click chemistry reagent, it contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups.
- Formula: C10H11NO5
- Molecular Weight: 225.20
Propargyl-PEG1-NHS ester is a nonclaevable 1-unit PEG linker for antibody-agent-conjugation (ADC). Propargyl-PEG1-NHS ester 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: C10H14N4O4
- Molecular Weight: 254.24
N3-C5-NHS ester is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N3-C5-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: C25H21N2NaO8S
- Molecular Weight: 532.50
DBCO-Sulfo-NHS ester sodium is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-Sulfo-NHS ester (sodium) 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: C27H46N4O7S
- Molecular Weight: 570.74
TCO-PEG3-Biotin is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). TCO-PEG3-Biotin is a click chemistry reagent, it contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups.
- Formula: C13H20N4O7
- Molecular Weight: 344.32
N3-PEG3-C2-NHS ester is a nonclaevable 3-unit PEG linker used in the synthesis of antibody-drug conjugates (ADCs). N3-PEG3-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: C12H23N7O5
- Molecular Weight: 345.35
Gly-Gly-Gly-PEG2-azide is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Gly-Gly-Gly-PEG4-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: C86H124N12O18
- Molecular Weight: 1613.97
DBCO-(PEG)3-VC-PAB-MMAE is a agent-linker conjugate for ADC. DBCO-(PEG)3-VC-PAB-MMAE is made by Monomethyl auristatin E (HY-15162) conjugats to DBCO-(PEG)3-vc-PAB linker. DBCO-(PEG)3-VC-PAB-MMAE can be used for the research of cancer. DBCO-(PEG)3-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: C14H30N4O6
- Molecular Weight: 350.41
Azido-PEG6-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG6-amine is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG6-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: C10H21N3O5
- Molecular Weight: 263.29
Azido-PEG5-alcohol is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG5-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG5-alcohol 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: C16H34N4O7
- Molecular Weight: 394.46
Azido-PEG7-amine is a non-cleavable 7 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG7-amine is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG7-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: C25H49N9O9
- Molecular Weight: 619.71
NH2-C5-PEG4-N3-L-Lysine-PEG3-N3 is a cleavable 7 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). NH2-C5-PEG4-N3-L-Lysine-PEG3-N3 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: C39H27N3O6S
- Molecular Weight: 665.71
Fluorescein-DBCO is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fluorescein-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: C61H58FN9O12
- Molecular Weight: 1128.16
DIBAC-GGFG-NH2CH2-Dxd (compound LP4), a Camptothecin (HY-16560) derivative, is a linker-payload of protein-agent conjugates. Dxd (HY-13631D) can be used as a payload for the antibody-coupling drug ADC (DS-8201a).DIBAC-GGFG-NH2CH2-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.
