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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bis-PEG2-endo-BCN

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

  • CAS Number: 1476737-97-9
  • MF: C28H40N2O6
  • MW: 500.63
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG25-NHS ester

Bis-PEG25-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2221948-96-3
  • MF: C14H16N2O10
  • MW: 372.28
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG3-Val-Cit-PAB-PNP

Azido-PEG3-Val-Cit-PAB-PNP is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Azido-PEG3-Val-Cit-PAB-PNP is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].

  • CAS Number: 2055047-18-0
  • MF: C34H47N9O12
  • MW: 773.79
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Maleimide-DOTA

Maleimide-DOTA is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 1006711-90-5
  • MF: C22H34N6O9
  • MW: 526.54
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AmPEG6C2-Aur0131

AmPEG6C2-Aur0131 is a non-cleavable anti-CXCR4 drug-linker conjugates for ADC.

  • CAS Number: 1650569-94-0
  • MF: C54H92N6O15
  • MW: 1065.34
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Boc-N-methyl-D-Valaldehyde

N-Boc-N-methyl-D-Valaldehyde is an ADC linker with a BOC protecting group.

  • CAS Number: 2165540-24-7
  • MF: C11H21NO3
  • MW: 215.28934
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Exatecan Intermediate 2

Exatecan Intermediate 2 (compound B) 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: 182182-31-6
  • MF: C13H15FN2O2
  • MW: 250.27
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-amido-(CH2COOH)2

Mal-amido-(CH2COOH)2, compound 7a, is a maleimidoethyl-containing intermediate for hydrophilic ADC linker[1].

  • CAS Number: 207613-14-7
  • MF: C11H12N2O7
  • MW: 284.22
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-Asn-Pro-Val-PABC-PNP

Fmoc-Asn-Pro-Val-PABC-PNP (compound 6) is a potent ADC Linker[1].

  • CAS Number: 2893871-64-0
  • MF: C43H44N6O11
  • MW: 820.84
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EC089

EC089 is a linker used in conjugates of tubulysins and folates, and extracted from patent WO2011069116A1[1].

  • CAS Number: 625827-91-0
  • MF: C36H46N14O14S
  • MW: 930.90
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG4-CH2CH2-Boc

Propargyl-PEG4-CH2CH2-Boc is a PEG- and Alkyl/ether-based non-cleavable ADC linker. Propargyl-PEG5-Boc can used to synthesize ADC inhibitors of Galectin-3[1].

  • CAS Number: 1245823-50-0
  • MF: C18H32O7
  • MW: 360.443
  • Catalog: ADC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 420.6±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 179.0±27.4 °C

Fmoc-Hyp(Bom)-OH

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

  • CAS Number: 187223-15-0
  • MF: C28H33N3O8
  • MW: 539.577
  • Catalog: ADC Linker
  • Density: 1.35±0.1 g/cm3
  • Boiling Point: 749.0±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 406.8±32.9 °C

DC44

DC44, a ADC cytotoxin, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC44 can be used for the targeted treatment of cancer[1].

  • CAS Number: 1354787-77-1
  • MF: C37H35ClN5O7PS
  • MW: 760.19
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG10-OH

Amino-PEG10-OH is non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 129449-09-8
  • MF: C20H43NO10
  • MW: 457.556
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 533.3±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 276.3±28.7 °C

m-PEG8-Ms

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

  • CAS Number: 1059588-19-0
  • MF: C18H38O11S
  • MW: 462.55
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L-Valine,N-[(1,1-dimethylethoxy)carbonyl]-N-methyl-, methyl ester

NSC 135130 (compound 11a) is a BOC-protected ADC linker that can be linked to tubulin-targeting inhibitors.Can be used to synthesize drug conjugates[1].

  • CAS Number: 24164-06-5
  • MF: C12H23NO4
  • MW: 245.31500
  • Catalog: ADC Linker
  • Density: 1.015g/cm3
  • Boiling Point: 293.5ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 131.3ºC

DC44SMe

DC44SMe, a phosphate prodrug of cytotoxic DNA alkylator DC44, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC44SMe exhibits IC50s of 2.0 nM, 2.8 nM, and 1.9 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC44SMe can be used for the targeted treatment of cancer[1].

  • CAS Number: 1354787-76-0
  • MF: C38H37ClN5O7PS2
  • MW: 806.29
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(5-Hydroxypentyl)maleimide

N-(5-Hydroxypentyl)maleimide is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs), such as Gemcitabine-O-Si(di-iso)-O-Mc (HY-130812) )[1].

  • CAS Number: 180608-78-0
  • MF: C9H13NO3
  • MW: 183.20
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-sar-oh

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

  • CAS Number: 154024-76-7
  • MF: C13H21N3O4S
  • MW: 315.388
  • Catalog: ADC Linker
  • Density: 1.3±0.0 g/cm3
  • Boiling Point: 646.1±0.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 344.5±0.0 °C

Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Br

Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Br is an ADC linker that can be used as a reaction reagent for the synthesis of anti-CD40 antibody agent conjugates (ADCs)[1].

  • CAS Number: 2345733-40-4
  • MF: C43H49BrF2N3O12P
  • MW: 948.74
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MP-PEG8-VA-PABC

MP-PEG8-VA-PABC is a protease cleavable ADC linker which is used in the treatment of several cancers[1].

  • CAS Number: 1938099-52-5
  • MF: C75H103N9O23
  • MW: 1498.67
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-Gly-NH-CH2-O-Cyclopropane-CH2COOH

Fmoc-Gly-NH-CH2-O-Cyclopropane-CH2COOH is an intermediate in the synthesis of ADC linker.The linker composed of Benzyl 2-cyclopropyl-2-hydroxyacetate can be coupled to Exatecan (HY-13631) and combined with antibodies (such as antibody hu2F7)[1].

  • CAS Number: 2414254-47-8
  • MF: C23H24N2O6
  • MW: 424.45
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Br-PEG4-C2-Boc

Br-PEG4-C2-Boc is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 564476-32-0
  • MF: C15H29BrO6
  • MW: 385.29100
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Boc-N-bis(PEG2-OH)

N-Boc-N-bis(PEG2-OH) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 275385-03-0
  • MF: C13H27NO6
  • MW: 293.36
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dimethylamine-SPDB

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

  • CAS Number: 1193111-73-7
  • MF: C15H19N3O4S2
  • MW: 369.46
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NO2-SPDMV

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

  • CAS Number: 663598-98-9
  • MF: C15H17N3O6S2
  • MW: 399.44
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG8-bromide

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

  • CAS Number: 2055046-25-6
  • MF: C19H35BrO8
  • MW: 471.38
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG4-C2-acid

Propargyl-PEG5-acid is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG5-acid can used to synthesize ADC inhibitors of Galectin-3[1].

  • CAS Number: 1245823-51-1
  • MF: C14H24O7
  • MW: 304.33600
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-amido-PEG8-val-gly-PAB-OH

Mal-amido-PEG8-val-gly-PAB-OH is a cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2353409-52-4
  • MF: C40H63N5O15
  • MW: 853.95
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Acetylene-linker-Val-Cit-PABC-MMAE

Acetylene-linker-Val-Cit-PABC-MMAE consists the ADCs linker (Acetylene-linker-Val-Cit-PABC) and potent tubulin inhibitor (MMAE), Acetylene-linker-Val-Cit-PABC-MMAE is an antibody drug conjugate.

  • CAS Number: 1411977-95-1
  • MF: C67H106N10O16
  • MW: 1307.616
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 1312.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 747.3±34.3 °C