Antibody-drug conjugates (ADCs) consist of a desirable monoclonal antibody, an active cytotoxic drug and an appropriate linker. An appropriate linker between the antibody and the cytotoxic drug provides a specific bridge, and thus helps the antibody to selectively deliver the cytotoxic drug to tumor cells and accurately releases the cytotoxic drug at tumor sites. In addition to conjugation, the linkers maintain ADCs’ stability during the preparation and storage stages of the ADCs and during the systemic circulation period. The ADCs currently undergoing clinical evaluation contain linkers are mostly classified into two categories: cleavable and noncleavable. Cleavable linkers rely on processes inside the cell to liberate the toxin, such as reduction in the cytoplasm, exposure to acidic conditions in the lysosome, or cleavage by specific proteases within the cell. Noncleavable linkers require proteolytic degradation of the antibody portion of the ADC for release of the cytotoxic molecule, which will retain the linker and the amino acid by which it was attached to the antibody. The selection of linker is target dependent, based on the knowledge of the internalization and degradation of the antibody-target antigen complex, and a preclinical in vitro and in vivo activity comparison of conjugates. Moreover, the choice of a linker is also influenced by which cytotoxin is used, as each molecule has different chemical constraints, and frequently the drug structure lends itself to a specific linker.


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PPA

PPA is an ADC linker (US20060073528A1). PPA can be used for making antibody-drug conjugate[1].

  • CAS Number: 452072-22-9
  • MF: C10H13NO2S2
  • MW: 243.35
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MAC glucuronide linker-1

MAC glucuronide linker-1 is a nonclaevable ADC linker for antibody-drug-conjugations (ADCs)[1].

  • CAS Number: 2222981-71-5
  • MF: C42H47N3O17S
  • MW: 897.90
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG4-Val-Cit-PAB-OH

Mal-PEG4-Val-Cit-PAB-OH is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2055041-39-7
  • MF: C33H50N6O11
  • MW: 706.78
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-Azidopropionic Acid Sulfo-NHS Ester

3-Azidopropionic Acid Sulfo-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2055198-09-7
  • MF: C7H7N4NaO7S
  • MW: 314.21
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG13-NHS ester

Bis-PEG13-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2221949-00-2
  • MF: C38H64N2O21
  • MW: 884.92
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-NH-ethyl-SS-propionic acid

Mal-NH-ethyl-SS-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2128735-24-8
  • MF: C12H16N2O5S2
  • MW: 332.40
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(2-pyridyldithio)-PEG1-hydrazine

(2-pyridyldithio)-PEG1-hydrazine is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 111625-28-6
  • MF: C7H9NOS2
  • MW: 187.283
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 323.3±38.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 149.3±26.8 °C

Fmoc-8-amino-3,6-dioxaoctanoic acid

Fmoc-8-amino-3,6-dioxaoctanoic acid (Fmoc-NH-PEG2-CH2COOH) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 166108-71-0
  • MF: C21H23NO6
  • MW: 385.410
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 631.4±45.0 °C at 760 mmHg
  • Melting Point: 90-92℃
  • Flash Point: 335.6±28.7 °C

Propargyl-PEG1-SS-alcohol

Propargyl-PEG1-SS-alcohol is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1391914-41-2
  • MF: C7H12O2S2
  • MW: 192.299
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 319.2±32.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 146.8±25.1 °C

Propargyl-PEG5-amine

Propargyl-PEG5-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG5-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 1589522-46-2
  • MF: C13H25NO5
  • MW: 275.341
  • Catalog: ADC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 360.4±37.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 166.5±20.2 °C

Ald-Ph-amido-PEG11-C2-NH2

Ald-Ph-amido-PEG11-C2-NH2 is a non-cleavable 11 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1337889-01-6
  • MF: C32H56N2O13
  • MW: 676.79
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG1-NHS ester

Mal-PEG1-NHS ester is a cleavable and PEG-based ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 1807518-72-4
  • MF: C13H14N2O7
  • MW: 310.259
  • Catalog: ADC Linker
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 488.4±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 249.2±31.5 °C

SIA Crosslinker

SIA Crosslinker is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 39028-27-8
  • MF: C6H6INO4
  • MW: 283.021
  • Catalog: ADC Linker
  • Density: 2.1±0.1 g/cm3
  • Boiling Point: 315.6±44.0 °C at 760 mmHg
  • Melting Point: 148ºC
  • Flash Point: 144.7±28.4 °C

Me-Tet-PEG4-NHBoc

Me-Tet-PEG4-NHBoc is an ADC Linker containing 4 PEG units. Me-Tet-PEG4-NHBoc can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups.

  • CAS Number: 2143955-71-7
  • MF: C26H40N6O7
  • MW: 548.63
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG3-Amine

m-PEG3-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 74654-07-2
  • MF: C7H17NO3
  • MW: 163.21500
  • Catalog: ADC Linker
  • Density: 0.978g/cm3
  • Boiling Point: 223.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 86.1ºC

Succinic anhydride

Succinic anhydride is a cyclic anhydride and an ADC linker extracted from patent WO2009064913A1. It can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide[1].

  • CAS Number: 108-30-5
  • MF: C4H4O3
  • MW: 100.073
  • Catalog: ADC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 261.0±0.0 °C at 760 mmHg
  • Melting Point: 118-120 °C(lit.)
  • Flash Point: 122.1±15.9 °C

MP-Ala-Ala-PAB

MP-Ala-Ala-PAB is a cleavable ADC Linker (ADC Linker). Fmoc-Ala-Ala-PAB can be used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1949793-47-8
  • MF: C20H24N4O6
  • MW: 416.43
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azidoethyl-SS-propionic acid

Azidoethyl-SS-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2228857-32-5
  • MF: C5H9N3O2S2
  • MW: 207.27
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG6-NHS ester

Propargyl-PEG6-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2093153-99-0
  • MF: C20H31NO10
  • MW: 445.46
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-N-(2-Boc-aminoethyl)-Gly-OH

Fmoc-N-(2-Boc-aminoethyl)-Gly-OH is a Fmoc-protected glycine derivative that can be used in antibody drug coupling (ADC) synthesis. ADC consists of antibodies that are linked to ADC cytotoxins via ADC junctions[1].

  • CAS Number: 141743-15-9
  • MF: C24H28N2O6
  • MW: 440.48900
  • Catalog: ADC Linker
  • Density: 1.25 g/cm3
  • Boiling Point: 638.3ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 339.8ºC

Tetraethylene glycol monotosylate

Tetraethylene glycol monotosylate is a cleavable and acylhydrazone-based ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 77544-60-6
  • MF: C15H24O7S
  • MW: 348.41200
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-Val-Cit-PAB-PNP

Boc-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 870487-10-8
  • MF: C30H40N6O10
  • MW: 644.6728
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG8-Amine

m-PEG8-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 869718-81-0
  • MF: C17H37NO8
  • MW: 383.47800
  • Catalog: ADC Linker
  • Density: 1.054
  • Boiling Point: 448ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 213.9ºC

Mal-amido-PEG8-acid

Mal-amido-PEG8-acid (example 143) is an ADC linker, extracted from patent US2018339985[1].

  • CAS Number: 1334177-86-4
  • MF: C26H44N2O13
  • MW: 592.63300
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Aminooxy-PEG4-alcohol

Aminooxy-PEG4-alcohol is a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Aminooxy-PEG4-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].

  • CAS Number: 106492-60-8
  • MF: C8H19NO5
  • MW: 209.24000
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MethylCBI-azaindole-benzamide-MOM-Boc-ethylenediamine-D

MethylCBI-azaindole-benzamide-MOM-Boc-ethylenediamine-D is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2222445-87-4
  • MF: C44H51ClN6O10
  • MW: 859.36
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-ethyl-SS-PEG3-NHBoc

Amino-ethyl-SS-PEG3-NHBoc is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2144777-87-5
  • MF: C15H32N2O5S2
  • MW: 384.55
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG4-Val-Cit-PAB

Mal-PEG4-Val-Cit-PAB is a cleavable ADC linker containing a Maleimide group. Mal-PEG4-Val-Cit-PAB is used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1949793-41-2
  • MF: C36H55N7O12
  • MW: 777.86
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-Hyp-OMe

Boc-Hyp-OMe is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Boc-Hyp-OMe is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].

  • CAS Number: 74844-91-0
  • MF: C11H19NO5
  • MW: 245.272
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 335.2±42.0 °C at 760 mmHg
  • Melting Point: 92-96 °C(lit.)
  • Flash Point: 156.6±27.9 °C

Gly-Gly-Gly-PEG4-methyltetrazine

Gly-Gly-Gly-PEG4-methyltetrazine is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2353409-82-0
  • MF: C23H34N8O7
  • MW: 534.57
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A