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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CCK2R Ligand-Linker Conjugates 1

CCK2R ligand CRL is a ligand-linker conjugate; which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker[1].

  • CAS Number: 1452145-13-9
  • MF: C72H110N12O27S
  • MW: 1607.77
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG4-PFP ester

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

  • CAS Number: 1334172-58-5
  • MF: C27H36F5N3O8S
  • MW: 657.647
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 804.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 440.6±34.3 °C

Aminooxy-PEG2-azide

Aminooxy-PEG2-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Aminooxy-PEG2-azide is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 1043426-13-6
  • MF: C6H14N4O3
  • MW: 190.20
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Me-Tet-PEG2-NHS

Me-Tet-PEG2-NHS is an ADC Linker containing 2 PEG units. Me-Tet-PEG2-NHS can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups.

  • CAS Number: 2740357-12-2
  • MF: C23H28N6O7
  • MW: 500.50
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dxd

Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).

  • CAS Number: 1599440-33-1
  • MF: C26H24FN3O6
  • MW: 493.48
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH2-PEG6-Boc

NH2-PEG6-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. NH2-PEG6-Boc is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 1286281-32-0
  • MF: C19H39NO8
  • MW: 409.51500
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH2-PEG9-acid

NH2-PEG9-acid is a non-cleavable 9 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 756526-04-2
  • MF: C19H39NO10
  • MW: 441.514
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 547.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 284.7±30.1 °C

Fmoc-N-amido-PEG8-acid

Fmoc-NH-PEG8-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 756526-02-0
  • MF: C34H49NO12
  • MW: 663.75200
  • Catalog: ADC Linker
  • Density: 1.190±0.06 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DOXO-EMCH

DOXO-EMCH is a 6-maleimidocaproyl hydrazone derivative of Doxorubicin, is an albumin binding prodrug.

  • CAS Number: 151038-96-9
  • MF: C37H42N4O13
  • MW: 750.74800
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-Azidopropionic Acid Sulfo-NHS Ester

3-Azidopropionic Acid Sulfo-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2055198-09-7
  • MF: C7H7N4NaO7S
  • MW: 314.21
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG13-NHS ester

Bis-PEG13-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2221949-00-2
  • MF: C38H64N2O21
  • MW: 884.92
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG3-Amine

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

  • CAS Number: 74654-07-2
  • MF: C7H17NO3
  • MW: 163.21500
  • Catalog: ADC Linker
  • Density: 0.978g/cm3
  • Boiling Point: 223.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 86.1ºC

Azidoethyl-SS-propionic acid

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

  • CAS Number: 2228857-32-5
  • MF: C5H9N3O2S2
  • MW: 207.27
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG6-NHS ester

Propargyl-PEG6-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2093153-99-0
  • MF: C20H31NO10
  • MW: 445.46
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Maytansinoid dM4

Maytansinoid DM4 is a thiol-containing maytansine derivative with highly potent cytotoxicity. Maytansinoid DM4 can be used as a cytotoxic moiety of ADC[1][2].

  • CAS Number: 799840-96-3
  • MF: C39H56ClN3O10S
  • MW: 794.394
  • Catalog: ADC Cytotoxin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 940.2±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 522.4±34.3 °C

Amino-ethyl-SS-PEG3-NHBoc

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

  • CAS Number: 2144777-87-5
  • MF: C15H32N2O5S2
  • MW: 384.55
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Puwainaphycin F

Puwainaphycin F, a cyanobacterial cyclic lipopeptide, is a moderate cytotoxin isolated from the soil cyanobacterium Cylindrospermum alatosporum C24/89. Puwainaphycin F causes necrotic cell death to mammalian cells via cell membrane permeabilization and subsequent unusual actin relocalization[1].

  • CAS Number: 1379577-47-5
  • MF: C53H87N13O15
  • MW: 1146.34
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-C-tri(CH2-PEG1-NHSester)

m-C-tri(CH2-PEG1-NHS ester) is a non-cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 173414-89-6
  • MF: C26H33N3O15
  • MW: 627.55
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG5-CH2CO2H

Azido-PEG5-CH2CO2H is a cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 217180-81-9
  • MF: C12H23N3O7
  • MW: 321.327
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ethyl 3-azetidinecarboxylate hydrochloride (1:1)

Ethyl azetidine-3-carboxylate hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Ethyl azetidine-3-carboxylate hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2]

  • CAS Number: 405090-31-5
  • MF: C6H12ClNO2
  • MW: 165.618
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Aminooxy-amido-PEG4-propargyl

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

  • CAS Number: 2253965-03-4
  • MF: C13H24N2O6
  • MW: 304.34
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

(rac)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer[1][2].

  • CAS Number: 102978-40-5
  • MF: C13H13NO5
  • MW: 263.25
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

mDPR-Val-Cit-PAB-MMAE

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

  • CAS Number: 1491152-26-1
  • MF: C65H100N12O15
  • MW: 1289.561
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 1353.3±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 772.3±34.3 °C

BS3 Crosslinker

BS3 Crosslinker is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 82436-77-9
  • MF: C16H20N2O14S2
  • MW: 550.447
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: >300°C
  • Flash Point: N/A

m-PEG6-CH2CH2CHO

m-PEG6-CH2CH2CHO is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 1058691-77-2
  • MF: C16H32O8
  • MW: 352.421
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 424.7±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 182.2±27.4 °C

MMAF sodium

MMAF sodium (Monomethylauristatin F sodium) is an antitubulin agent that inhibit cell division; attenuates its cytotoxic activity compared to MMAE. MMAF sodium is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.

  • CAS Number: 1799706-65-2
  • MF: C39H64N5NaO8
  • MW: 753.94
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SCO-PEG3-Maleimide

SCO-PEG3-Maleimide is a cleavable ADC Linker containing 3 PEG units. SCO-PEG3-Maleimide can be used as a copper-free click chemical reagent for catalyst-free click reactions. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.

  • CAS Number: 2141976-35-2
  • MF: C24H35N3O8
  • MW: 493.55
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG6-azide

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

  • CAS Number: 1043884-49-6
  • MF: C13H27N3O6
  • MW: 321.37000
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Me-Tet-PEG4-Maleimide

Me-Tet-PEG4-Maleimide is an ADC Linker containing 4 PEG units. Me-Tet-PEG4-Maleimide can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.

  • CAS Number: 1715913-76-0
  • MF: C28H37N7O8
  • MW: 599.64
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Corixetan

Corixetan is a highly efficient thorium chelator. Corixetan can efficiently complex Th-227 with sufficient in vivo stability[1].

  • CAS Number: 1952359-26-0
  • MF: C50H61N11O15
  • MW: 1056.08
  • Catalog: ADC Cytotoxin
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 1320.8±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 752.6±34.3 °C