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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m-PEG9-Amine

m-PEG9-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 211859-73-3
  • MF: C19H41NO9
  • MW: 427.53000
  • Catalog: ADC Linker
  • Density: 1.06
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Gly-Cyclopropane-Exatecan

Gly-Cyclopropane-Exatecan involves in the synthesis of anti-B7-H4 ADC, containing Exatecan (HY-13631), a DNA Topoisomerase I inhibitor. Gly-Cyclopropane-Exatecan participated in the formation of the ADC hu2F7-Exatecan (compound 34), which showed antitumor activity in vivo and in vitro[1].

  • CAS Number: 2414254-49-0
  • MF: C32H34FN5O7
  • MW: 619.64
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SC209 intermediate-1

SC209 intermediate-1 (Compound A7a) is an ADC linker. SC209 intermediate-1 can be used for synthesis of ADCs[1].

  • CAS Number: 1977557-93-9
  • MF: C21H30N2O6
  • MW: 406.47
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tetrazine-SS-Biotin

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

  • CAS Number: 2123482-78-8
  • MF: C24H32N8O3S3
  • MW: 576.76
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N3-D-Orn(Boc)-OH

N3-D-Orn(Boc)-OH is a Boc-protected pentanoic amino acid derivative, can be used as a click chemistry reagent and has been used to synthesis antibody-drug conjugates (ADC)[1].

  • CAS Number: 2165877-62-1
  • MF: C10H18N4O4
  • MW: 258.27
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Acid-C3-SSPy

Acid-C3-SSPy is a cleavable DBA-DM4 linker used in the synthesis of DBA-DM4 (HY-128960), a drug-linker conjugate for ADC[1].

  • CAS Number: 250266-79-6
  • MF: C9H11NO2S2
  • MW: 229.319
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 411.6±41.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 202.7±27.6 °C

L-Ornithinamide, N-[[2-[2-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)ethoxy]ethoxy]carbonyl]-L-valyl-N5-(aminocarbonyl)-N-[4-[[[(4-nitrophenoxy)carbonyl]oxy]methyl]phenyl]-

Mal-PEG2-Val-Cit-PABA-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1345681-52-8
  • MF: C34H41N7O13
  • MW: 755.73
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-BOC-AZETIDINE-3-CARBOXYLICACIDMETHYLESTER

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

  • CAS Number: 610791-05-4
  • MF: C10H17NO4
  • MW: 215.246
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 269.0±33.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 116.5±25.4 °C

tans-4-Hydroxy-D-proline hydrochloride

tans-4-Hydroxy-D-proline hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). tans-4-Hydroxy-D-proline hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PR

  • CAS Number: 142347-81-7
  • MF: C5H10ClNO3
  • MW: 167.591
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: 368.6ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 176.7ºC

Fmoc-Lys-OH hydrochloride

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

  • CAS Number: 139262-23-0
  • MF: C21H25ClN2O4
  • MW: 404.887
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: 607.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 321.3ºC

MC-VC-PABC-DNA31

MC-VC-PABC-DNA31 has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-VC-PABC-DNA31 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: 1639352-03-6
  • MF: C77H94N10O21
  • MW: 1495.62
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

diSPhMC-Asn-Pro-Val-PABC-MMAE

diSPhMC-Asn-Pro-Val-PABC-MMAE (compound 9) is a potent ADC Linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2893871-68-4
  • MF: C83H115N11O16S2
  • MW: 1587.00
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate

S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate is a glutathione cleavable ADC linker used for the antibody-drug conjugates (ADCs) and refers to the Alkyl-Chain composition. S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate is the linker portions of the molecules employed for mAb attachment purposes[1].

  • CAS Number: 2127875-65-2
  • MF: C5H12O3S2
  • MW: 184.28
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG10-amine

m-PEG10-amine is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. m-PEG10-amine is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1383658-09-0
  • MF: C21H45NO10
  • MW: 471.583
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 518.9±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 254.4±22.4 °C

Tr-PEG3-OH

Tr-PEG3-OH is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 133699-09-9
  • MF: C25H28O4
  • MW: 392.48700
  • Catalog: ADC Linker
  • Density: 1.126±0.06 g/cm3(Predicted)
  • Boiling Point: 521.8±45.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG4-VC-PAB-DMEA

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

  • CAS Number: 1569261-93-3
  • MF: C41H65N9O13
  • MW: 892.01
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Me-triacetyl-β-D-glucopyranuronate-Ph-ald-NO2

Me-triacetyl-β-D-glucopyranuronate-Ph-ald-NO2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 148579-93-5
  • MF: C20H21NO13
  • MW: 483.380
  • Catalog: ADC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 582.6±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 219.6±32.1 °C

Asn-Pro-Val-PABC-MMAE TFA

Asn-Pro-Val-PABC-MMAE TFA (compound 8) is a potent ADC Linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2893871-67-3
  • MF: C63H97F3N10O15
  • MW: 1291.50
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-Val-Ala-PAB

Boc-Val-Ala-PAB is a cathepsin cleavable ADC linker that is used for making antibody-drug conjugate (ADCs)[1][2].

  • CAS Number: 1884577-99-4
  • MF: C20H31N3O5
  • MW: 393.48
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG3-acid

Propargyl-PEG3-acid is a non-cleavable (3 unit PEG) ADC linker and also a PEG-based PROTAC linker that can be used to synthesis 6-OHDA-PEG3-yne. 6-OHDA-PEG3-yne contains 6-OHDA (HY-B1081, HY-B1081A) and Propargyl-PEG3-acid[1].

  • CAS Number: 1347760-82-0
  • MF: C10H16O5
  • MW: 216.231
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 348.0±32.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 131.8±18.6 °C

SPDB-DM4

SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4) via a SPDB linker, exhibiting potent anti-tumor activity.

  • CAS Number: 1626359-62-3
  • MF: C46H63ClN4O14S2
  • MW: 995.59
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BCN-PEG4-HyNic

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

  • CAS Number: 1507370-54-8
  • MF: C28H41N5O6
  • MW: 543.66
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AcLys-PABC-VC-Aur0101

AcLys-PABC-VC-Aur0101 is a cleavable anti-CXCR4 drug-linker conjugates for ADC.

  • CAS Number: 1438851-17-2
  • MF: C66H103N13O13S
  • MW: 1318.67
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-Gly-Gly-allyl propionate

Fmoc-Gly-Gly-allyl propionate is a cleavable linker that can be used to synthesize Antibody-Drug Conjugates (ADCs).

  • CAS Number: 2766214-15-5
  • MF: C25H26N2O7
  • MW: 466.48
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-Val-Ala-aminomethyl acetate

Fmoc-Val-Ala-aminomethyl acetate (Compound 58b) is an ADC Linker, and can be used for synthesis of ADCs[1].

  • CAS Number: 2505045-86-1
  • MF: C26H31N3O6
  • MW: 481.54
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Maleic anhydride-1,4-13C2

Succinic anhydride-13C2 is the 13C labeled Succinic anhydride[1]. Succinic anhydride is a cyclic anhydride and a nonclaevable ADC linker extracted from patent WO2009064913A1. Succinic anhydride can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide[2].

  • CAS Number: 67519-25-9
  • MF: C4H4O3
  • MW: 102.05800
  • Catalog: ADC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ald-CH2-PEG3-azide

Ald-CH2-PEG3-azide is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1002342-83-7
  • MF: C8H15N3O4
  • MW: 217.22200
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ald-CH2-PEG5-azide

Ald-CH2-PEG5-azide is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1446282-38-7
  • MF: C12H23N3O6
  • MW: 305.328
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MMAD

MMAD is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugates (ADCs).

  • CAS Number: 203849-91-6
  • MF: C41H66N6O6S
  • MW: 771.064
  • Catalog: ADC Cytotoxin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 906.1±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 501.8±34.3 °C

SC239

SC239 is a cleavable 2-aminophenyl hemiasterlin drug-linker. SC239 can be as the drug-linker for ADC[1].

  • CAS Number: 1977557-97-3
  • MF: C65H84N10O11
  • MW: 1181.42
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A