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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NHS-SS-Ph

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

  • CAS Number: 2750799-12-1
  • MF: C16H17NO7S2
  • MW: 399.44
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-amido-PEG3-C1-PFP ester

Mal-amido-PEG3-C1-PFP ester is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2101206-13-5
  • MF: C21H21F5N2O8
  • MW: 524.39
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG1-SS-PEG1-PFP ester

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

  • CAS Number: 1817735-30-0
  • MF: C16H15F5O4S2
  • MW: 430.41
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sulfo-SPP sodium

Sulfo-SPP sodium a heterobifunctional, thiol-cleavable and membrane impermeable crosslinker.

  • CAS Number: 452072-24-1
  • MF: C14H15N2NaO7S3
  • MW: 442.46
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG1-SS-PEG1-C2-Boc

Propargyl-PEG1-SS-PEG1-C2-Boc is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1807518-78-0
  • MF: C14H24O4S2
  • MW: 320.468
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 407.4±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 187.0±15.4 °C

Bis-SS-C3-NHS ester

Bis-SS-C3-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 98604-88-7
  • MF: C16H20N2O8S2
  • MW: 432.47
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DBCO-NHCO-PEG4-NH-Boc

DBCO-NHCO-PEG4-NH-Boc is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1255942-12-1
  • MF: C34H45N3O8
  • MW: 623.74
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-N-methyl-PEG3-CH2CH2COOH

Fmoc-N-methyl-PEG3-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1807518-77-9
  • MF: C25H31NO7
  • MW: 413.464
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 597.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 315.1±28.7 °C

Acid-PEG3-SS-PEG3-acid

Acid-PEG3-SS-PEG3-acid is a cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2055014-98-5
  • MF: C18H34O10S2
  • MW: 474.59
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tolytoxin

Tolytoxin, a bioactive metabolite from cyanobacteria, is a potent antifungal antibiotic, exhibiting MICs of 0.25-8 nmol. Tolytoxin is a cyanobacterial macrolide that targets actin by inhibition of its polymerization. Tolytoxin has cytotoxic effects in cancer cells[1].

  • CAS Number: 127999-44-4
  • MF: C46H75NO13
  • MW: 850.09
  • Catalog: Fungal
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PAC

PAC comprises an antibody conjugated via a linker to a PROTAC. PAC extracts from patent WO2017201449A1, compound PAC1. PAC is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).

  • CAS Number: 2158322-33-7
  • MF: C94H107N13O16
  • MW: 1674.93
  • Catalog: PROTAC-linker Conjugate for PAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-SS-C3-sulfo-NHS ester

Bis-SS-C3-sulfo-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 98604-89-8
  • MF: C16H20N2O14S4
  • MW: 592.60
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Campathecin

Campathecin is a potent DNA enzyme topoisomerase I inhibitor, with an IC50 of 679 nM.

  • CAS Number: 7689-03-4
  • MF: C20H16N2O4
  • MW: 348.352
  • Catalog: ADC Cytotoxin
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 757.0±60.0 °C at 760 mmHg
  • Melting Point: 260 °C (dec.)(lit.)
  • Flash Point: 411.6±32.9 °C

Docosanedioic acid

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

  • CAS Number: 505-56-6
  • MF: C22H42O4
  • MW: 370.566
  • Catalog: ADC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 527.0±23.0 °C at 760 mmHg
  • Melting Point: 72-80 °C(lit.)
  • Flash Point: 286.6±19.1 °C

Aeruginosin 865

Aeruginosin 865, isolated from terrestrial cyanobacterium Nostoc sp. Lukešová 30/93, is the first aeruginosin-type peptide containing both a fatty acid and a carbohydrate moiety. Aeruginosin 865 inhibits translocation of NF-kB to the nucleus. Aeruginosin 865 has anti-inflammatory effect[1]

  • CAS Number: 1611990-01-2
  • MF: C41H64N6O14
  • MW: 864.98
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Agrochelin

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

  • CAS Number: 247115-74-8
  • MF: C23H34N2O4S2
  • MW: 466.66
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG7-NHS ester

Bis-PEG7-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1334170-02-3
  • MF: C26H40N2O15
  • MW: 476.47488
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

sulfo-SPDB

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

  • CAS Number: 1193111-39-5
  • MF: C13H14N2O7S3
  • MW: 406.45
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DBCO acid 2

DBCO acid 2 is a Click Chemistry intermidate used for antibody-drug conjugates.

  • CAS Number: 1207355-31-4
  • MF: C20H17NO3
  • MW: 319.354
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 635.5±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 338.2±31.5 °C

sulfo-SPDB-DM4

sulfo-SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4) via the sulfo-SPDB linker.

  • CAS Number: 1626359-59-8
  • MF: C46H63ClN4O17S3
  • MW: 1075.66
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DBCO-NHCO-PEG4-acid

DBCO-Amide-PEG5-acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1870899-46-9
  • MF: C32H40N2O9
  • MW: 596.67
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dolastatin 15

Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin[1][2][3].

  • CAS Number: 123884-00-4
  • MF: C45H68N6O9
  • MW: 837.05600
  • Catalog: ADC Cytotoxin
  • Density: 1.2g/cm3
  • Boiling Point: 943.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 524.2ºC

N-Bromoacetyl-β-alanine

N-Bromoacetyl-β-alanine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]. N-Bromoacetyl-β-alanine is also a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 89520-11-6
  • MF: C5H8BrNO3
  • MW: 210.02600
  • Catalog: ADC Linker
  • Density: 1.682g/cm3
  • Boiling Point: 433.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 215.9ºC

Azido-PEG8-NHS ester

Azido-PEG8-NHS ester is a cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Azido-PEG8-NHS ester is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[2].

  • CAS Number: 1204834-00-3
  • MF: C23H40N4O12
  • MW: 564.58300
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG4-Val-Cit-PAB-PNP

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

  • CAS Number: 2112738-09-5
  • MF: C40H53N7O15
  • MW: 871.89
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydroxy-PEG3-SS-PEG3-alcohol

Hydroxy-PEG3-SS-PEG3-alcohol is also a cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 5662-81-7
  • MF: C16H34O8S2
  • MW: 293.33800
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DBCO-PEG5-NHS ester

DBCO-PEG4-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2144395-59-3
  • MF: C36H43N3O11
  • MW: 693.74
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4-Methyl-4-(methyldisulfanyl)pentanoicacid

4-Methyl-4-(methyldisulfanyl)pentanoic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 796073-55-7
  • MF: C7H14O2S2
  • MW: 194.31500
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

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