The antibody-drug conjugate (ADC), a humanized or human monoclonal antibody conjugated with highly cytotoxic small molecules (payloads) through chemical linkers, is a novel therapeutic format and has great potential to make a paradigm shift in cancer chemotherapy. The three components of the ADC together give rise to a powerful oncolytic agent capable of delivering normally intolerable cytotoxins directly to cancer cells, which then internalize and release the cell-destroying drugs. At present, two ADCs, Adcetris and Kadcyla, have received regulatory approval with >40 others in clinical development.

ADCs are administered intravenously in order to prevent the mAb from being destroyed by gastric acids and proteolytic enzymes. The mAb component of the ADC enables it to circulate in the bloodstream until it finds and binds to tumor-specific cell surface antigens present on target cancer cells. Linker chemistry is an important determinant of the safety, specificity, potency and activity of ADCs. Linkers are designed to be stable in the blood stream (to conform to the increased circulation time of mAbs) and labile at the cancer site to allow rapid release of the cytotoxic drug. First generation ADCs made use of early cytotoxins such as the anthracycline, doxorubicin or the anti-metabolite/antifolate agent, methotrexate. Current cytotoxins have far greater potency and can be divided into three main groups: auristatins, maytansines and calicheamicins.

The development of site-specific conjugation methodologies for constructing homogeneous ADCs is an especially promising path to improving ADC design, which will open the way for novel cancer therapeutics.

References:
[1] Tsuchikama K, et al. Protein Cell. 2016 Oct 14. DOI:10.1007/s13238-016-0323-0.
[2] Peters C, et al. Biosci Rep. 2015 Jun 12;35(4). pii: e00225. doi: 10.1042/BSR20150089.


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(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

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

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

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

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

Azidoethyl-SS-propionic NHS ester

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

  • CAS Number: 2243566-44-9
  • MF: C9H12N4O4S2
  • MW: 304.35
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-NH-ethyl-SS-propionic NHS ester

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

  • CAS Number: 2128735-23-7
  • MF: C24H24N2O6S2
  • MW: 500.59
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

alpha-Amanitin

alpha-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.

  • CAS Number: 23109-05-9
  • MF: C39H54N10O14S
  • MW: 918.97000
  • Catalog: ADC Cytotoxin
  • Density: 1.57 g/cm3
  • Boiling Point: 1622.2ºC at 760 mmHg
  • Melting Point: 254-255ºC(lit.)
  • Flash Point: 934.9ºC

Azidoethyl-SS-ethylamine

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

  • CAS Number: 1807512-40-8
  • MF: C4H10N4S2
  • MW: 178.28
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MDTF free acid

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

  • CAS Number: 2102021-49-6
  • MF: C16H11F4NO9S
  • MW: 469.32
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-amide-PEG8-Val-Ala-PAB-PNP

Mal-amide-PEG8-Val-Ala-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2210247-59-7
  • MF: C48H68N6O19
  • MW: 1033.08
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EGGGG-PEG8-amide-bis(deoxyglucitol)

EGGGG-PEG8-amide-bis(deoxyglucitol) is a cleavable ADC linker.

  • CAS Number: 2842855-38-1
  • MF: C49H91N9O28
  • MW: 1254.29
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MC-Sq-Cit-PAB-Gefitinib

MC-Sq-Cit-PAB-Gefitinib has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Sq-Cit-PAB-Gefitinib is used for the antibody-drug conjugates (ADC) to treat various diseases or disorders, e.g. characterized by the overexpression of a tumor antigen[1,2].

  • CAS Number: 1941168-63-3
  • MF: C50H61ClFN10O9
  • MW: 1000.53
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Doxorubicin-SMCC

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

  • CAS Number: 400647-59-8
  • MF: C39H42N2O14
  • MW: 762.76
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Gly-Gly-Gly-PEG3-TCO

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

  • CAS Number: 2353409-81-9
  • MF: C23H41N5O8
  • MW: 515.60
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG9-acid

Bis-​PEG9-​acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-​PEG9-​acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1268488-70-5
  • MF: C22H42O13
  • MW: 514.561
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 630.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 201.6±25.0 °C

Icosanedioic acid

Eicosanedioic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Eicosanedioic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis

  • CAS Number: 2424-92-2
  • MF: C20H38O4
  • MW: 342.513
  • Catalog: ADC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 504.1±23.0 °C at 760 mmHg
  • Melting Point: 127ºC
  • Flash Point: 272.8±19.1 °C

Boc-aminooxy-ethyl-SS-propanol

Boc-aminooxy-ethyl-SS-propanol is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2128735-21-5
  • MF: C9H19NO4S2
  • MW: 269.38
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Glucopiericidin A

Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts[1][2].

  • CAS Number: 108073-65-0
  • MF: C31H47NO9
  • MW: 577.70600
  • Catalog: ADC Cytotoxin
  • Density: 1.21g/cm3
  • Boiling Point: 735.8ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 398.8ºC

Tr-PEG6-OH

Tr-PEG6-OH is a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 127999-16-0
  • MF: C31H40O7
  • MW: 524.645
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 630.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 334.9±30.1 °C

Gly-Gly-Gly-PEG4-DBCO

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

  • CAS Number: 2353409-80-8
  • MF: C35H46N6O9
  • MW: 694.77
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-NH-PEG8-CH2COOH

Fmoc-NH-PEG8-CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 868594-52-9
  • MF: C33H47NO12
  • MW: 649.72600
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mc-Val-Cit-PAB-Cl

Mc-Val-Cit-PAB-Cl is an ADC linker. Mc-Val-Cit-PAB-Cl can be used to conjugate MMAE and antibody to form antibody-MC-vc-MMAE (e.g., anti-CD22-MC-VC-PABC-MMAE with IC50s of 3.3 and 0.95 nM for BJAB and WSU cell lines in cytotoxicity assay).

  • CAS Number: 1639351-92-0
  • MF: C28H39ClN6O6
  • MW: 591.10
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Duocarmycin A

Duocarmycin A, which is one of well-known antitumor antibiotics, efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels[1].

  • CAS Number: 118292-34-5
  • MF: C26H25N3O8
  • MW: 507.49200
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DSS Crosslinker

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

  • CAS Number: 68528-80-3
  • MF: C16H20N2O8
  • MW: 368.339
  • Catalog: ADC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 513.5±60.0 °C at 760 mmHg
  • Melting Point: 169-170ºC
  • Flash Point: 264.4±32.9 °C

1-benzyloxycarbonylazetidine-3-carboxylic acid

1-Cbz-azetidine-3-carboxylic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-Cbz-azetidine-3-carboxylic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]

  • CAS Number: 97628-92-7
  • MF: C12H13NO4
  • MW: 235.236
  • Catalog: ADC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 421.2±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 208.5±28.7 °C

m-PEG12-amine

m-PEG12-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. m-PEG12-amine is also a non-cleavable 12 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 1977493-48-3
  • MF: C25H53NO12
  • MW: 559.688
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 583.6±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 291.3±22.4 °C

Diacetyl Agrochelin

Diacetyl Agrochelin is an acetyl derivative of Agrochelin, which is produced by the fermentation of a marine Agrobacterium sp. Diacetyl Agrochelin has cytotoxic activity in tumor cell lines[1].

  • CAS Number: 247115-75-9
  • MF: C27H38N2O6S2
  • MW: 550.73
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mc-MMAE

Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate (ADC).

  • CAS Number: 863971-24-8
  • MF: C49H78N6O10
  • MW: 911.17800
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: 1.144±0.06 g/cm3(Predicted)
  • Boiling Point: 1025.2±65.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

β-D-glucuronide-pNP-carbonate

β-D-glucuronide-pNP-carbonate is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 894095-98-8
  • MF: C45H43N3O18
  • MW: 913.83
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A