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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NH-bis-PEG2

NH-bis-PEG2 is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 54384-47-3
  • MF: C8H19NO4
  • MW: 193.24
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MC-Val-Cit-PAB-vinblastine

MC-Val-Cit-PAB-vinblastine has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-vinblastine is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].

  • CAS Number: 2055896-92-7
  • MF: C74H97N10O15
  • MW: 1366.62
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S)-4-ethyl-4-hydroxy-7,8-dihydro-1H-pyrano[3,4-f]indolizine-3,6,10(4H)-trione

Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers[1][2].

  • CAS Number: 110351-94-5
  • MF: C13H13NO5
  • MW: 263.25
  • Catalog: ADC Cytotoxin
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 666.6±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 357.0±31.5 °C

Fmoc-NH-PEG5-CH2COOH

Fmoc-NH-PEG5-CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 635287-26-2
  • MF: C27H35NO9
  • MW: 517.56800
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AEEA-AEEA

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

  • CAS Number: 1143516-05-5
  • MF: C12H24N2O7
  • MW: 308.32800
  • Catalog: ADC Linker
  • Density: 1.202±0.06 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-Ala-Ala-PAB

Fmoc-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: 1384263-83-5
  • MF: C28H29N3O5
  • MW: 487.55
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG4-CH2-Boc

Azido-PEG4-CH2-Boc is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Azido-PEG4-CH2-Boc is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[2].

  • CAS Number: 864681-04-9
  • MF: C14H27N3O6
  • MW: 333.38100
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-trifluoroacetyl-β-alanyl chloride

N-trifluoroacetyl-β-alanyl chloride is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 87639-76-7
  • MF: C5H5ClF3NO2
  • MW: 203.54700
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG7-acid

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

  • CAS Number: 2093154-00-6
  • MF: C18H32O9
  • MW: 392.44
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NO2-SPP-sulfo

NO2-SPP-sulfo is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 663598-66-1
  • MF: C14H15N3O9S3
  • MW: 465.48
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Di-​tert-​butyl iminodiacetate

NH-bis(C1-Boc)is a uncleavable linker used for antibody-drug conjugates (ADC).

  • CAS Number: 85916-13-8
  • MF: C12H23NO4
  • MW: 245.315
  • Catalog: ADC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 298.0±25.0 °C at 760 mmHg
  • Melting Point: 38-42ºC(lit.)
  • Flash Point: 134.0±23.2 °C

Methyl azetidine-3-carboxylate hydrochloride

Methyl azetidine-3-carboxylate hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Methyl azetidine-3-carboxylate hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs<

  • CAS Number: 100202-39-9
  • MF: C5H10ClNO2
  • MW: 151.591
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: 190.9ºC at 760 mmHg
  • Melting Point: 93.0 to 97.0 °C
  • Flash Point: 69.3ºC

Boc-NH-PEG4-CH2CH2NH2

Boc-NH-PEG4-CH2CH2NH2 a cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 811442-84-9
  • MF: C15H32N2O6
  • MW: 336.42400
  • Catalog: ADC Linker
  • Density: 1.059
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: 222 °C

Fmoc-NH-PEG3-CH2CH2COOH

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

  • CAS Number: 867062-95-1
  • MF: C24H29NO7
  • MW: 443.490
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 651.9±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 348.0±31.5 °C

Me-Tet-PEG5-COOH

Me-Tet-PEG5-COOH is an ADC Linker containing 5 PEG units. Me-Tet-PEG5-COOH can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups.

  • CAS Number: 2143964-72-9
  • MF: C24H35N5O8
  • MW: 521.56
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MC-VC-PAB-NH2

MC-vc-PAB-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1616727-20-8
  • MF: C31H46N8O8
  • MW: 658.75
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SGD-1882

SGD-1882 is a cytotoxic, DNA minor-groove crosslinking agent pyrrolobenzodiazepine (PBD) dimer, acting as the payload for ADCs.

  • CAS Number: 1222490-34-7
  • MF: C42H39N5O7
  • MW: 725.788
  • Catalog: ADC Cytotoxin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 977.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 545.1±34.3 °C

NO2-SPDMV-sulfo

NO2-SPDMV-sulfo is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 663599-00-6
  • MF: C15H17N3O9S3
  • MW: 479.51
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-BOC-cis-4-Hydroxy-L-proline

N-Boc-cis-4-hydroxy-L-proline is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N-Boc-cis-4-hydroxy-L-proline is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2

  • CAS Number: 87691-27-8
  • MF: C10H17NO5
  • MW: 231.246
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 390.9±42.0 °C at 760 mmHg
  • Melting Point: 146ºC
  • Flash Point: 190.2±27.9 °C

MC-VC-PAB-NH2 TFA

MC-VC-PAB-NH2 TFA is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1616727-21-9
  • MF: C33H47F3N8O10
  • MW: 772.77
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG2-acid

Propargyl-PEG2-acid is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1859379-85-3
  • MF: C8H12O4
  • MW: 172.18
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Me-Tet-PEG9-COOH

Me-Tet-PEG9-COOH is an ADC Linker containing 9 PEG units. Me-Tet-PEG9-COOH can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups.

  • CAS Number: 2143964-70-7
  • MF: C32H51N5O12
  • MW: 697.77
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MC-Val-Cit-PAB-NH-C2-NH-Boc

MC-Val-Cit-PAB-NH-C2-NH-Boc is a cathepsin cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1616727-22-0
  • MF: C36H54N8O10
  • MW: 758.86
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG2-Amine

m-PEG2-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 31576-51-9
  • MF: C5H13NO2
  • MW: 119.162
  • Catalog: ADC Linker
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 163.7±15.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 54.1±27.7 °C

Biotin-PEG1-NH2

Biotin-PEG1-NH2 is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 811442-85-0
  • MF: C14H26N4O3S
  • MW: 330.45
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-EGGGG-PEG8-amide-bis(deoxyglucitol)

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

  • CAS Number: 2360920-01-8
  • MF: C55H94N10O31
  • MW: 1391.38
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-O-amido-C11-COOH

Thalidomide-O-amido-C11-COOH (compound IMiD acid 1) is an E3 ligase ligand and linker CRBN (Cereblon) conjugate. Thalidomide-O-amido-C11-COOH can be used to synthesize PROTAC that target the degradation of DOT1L[1].

  • CAS Number: 2473270-96-9
  • MF: C27H35N3O8
  • MW: 529.58
  • Catalog: PROTAC-linker Conjugate for PAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Boc-O-tosyl hydroxylamine

N-Boc-O-tosyl hydroxylamine is used as a linker for antibody-drug conjugates (ADC)[1].

  • CAS Number: 105838-14-0
  • MF: C12H17NO5S
  • MW: 287.33200
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Cbz-glycyl-glycyl-D-phenylalanine

N-Cbz-glycyl-glycyl-D-phenylalanine is a cleavable ADC linker.

  • CAS Number: 1802522-76-4
  • MF: C21H23N3O6
  • MW: 413.42
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BCN-endo-PEG7-NH2

BCN-endo-PEG7-NH2 is an ADC Linker containing 7 PEG units. BCN-endo-PEG7-NH2 contains the lyophilic bidentate macrocyclic ligand endo-BCN, which can further synthesize macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.

  • CAS Number: 2143968-34-5
  • MF: C27H48N2O9
  • MW: 544.68
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A