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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Me-Tet-PEG8-Maleimide

Me-Tet-PEG8-Maleimide is an ADC Linker containing 8 PEG units. Me-Tet-PEG8-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: 2143968-05-0
  • MF: C36H53N7O12
  • MW: 775.85
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-NH-PEG4-CH2COOH

Boc-NH-PEG4-CH2COOH is a cleavable ADC linker used as a linker for antibody-drug conjugates (ADC)[1].

  • CAS Number: 876345-13-0
  • MF: C15H29NO8
  • MW: 351.39300
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DC1-SMe

DC1-Sme is an antibody conjugate of phosphate prodrug of cytotoxic DNA alkylators for the targeted treatment of cancer.

  • CAS Number: 501666-85-9
  • MF: C35H30ClN5O4S2
  • MW: 684.23
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

McMMAF

Mc-MMAF is a protective group-conjugated MMAF. MMAF is a more potent drug than Monomethyl auristatin E (MMAE), but is charged and relatively membrane-impermeable, is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.Target:MMAF is a new auristatin derivative with a charged C-terminal phenylalanine that attenuates its cytotoxic activity compared to its uncharged counterpart, Monomethyl auristatin E (MMAE). Because of MMAF is highly toxic, it cannot be used as a drug itself. MMAF induces potent antitumor effects when conjugated via protease cleavable linkers to a monoclonal antibody targeting internalizing, tumor-specific cell surface antigens. The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the anti-mitotic mechanism.

  • CAS Number: 863971-19-1
  • MF: C49H76N6O11
  • MW: 925.161
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 1052.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 590.1±34.3 °C

6-Quinoxalinecarboxylic acid, 2,3-bis(bromomethyl)-

6-Quinoxalinecarboxylic acid, 2,3-bis(bromomethyl)- is an useful linker for antibody-drug-conjugations (ADCs), extracted from [Bioorg Chem. 2012 Apr-Jun;41-42:1-5.] compound 1i.

  • CAS Number: 32602-11-2
  • MF: C11H8Br2N2O2
  • MW: 360.001
  • Catalog: ADC Linker
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 437.3±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 218.3±27.3 °C

m-PEG4-Boc

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

  • CAS Number: 883554-11-8
  • MF: C14H28O6
  • MW: 292.36900
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

endo-BCN-Fmoc-L-Lysine

Endo-BCN-Fmoc-L-Lysine is a linker containing 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: 1493802-95-1
  • MF: C32H36N2O6
  • MW: 544.65
  • Catalog: ADC Linker
  • Density: 1.30±0.1 g/cm3(Predicted)
  • Boiling Point: 775.1±60.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG7-acid

Bis-PEG7-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-PEG6-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 94376-75-7
  • MF: C18H34O11
  • MW: 426.45600
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Z-AEVD-FMK

Z-AEVD-FMK is a cleavable ADC linker for the synthesis of antibody active molecule conjugates (ADCs).

  • CAS Number: 1135688-47-9
  • MF: C28H39FN4O10
  • MW: 610.628
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 883.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 488.3±34.3 °C

({N-[(9H-Fluoren-9-ylmethoxy)carbonyl]glycyl}amino)methyl acetate

Fmoc-Gly-NH-CH2-acetyloxy is a cleavable linker that can be used to synthesize antiboy-drug Conjugates (ADCs).

  • CAS Number: 1599440-06-8
  • MF: C20H20N2O5
  • MW: 368.38
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MCC-Modified Daunorubicinol

MC-VA-Modified PABC is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates[1].

  • CAS Number: 721945-30-8
  • MF: C39H44N4O13
  • MW: 776.79
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG1-PFP ester

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

  • CAS Number: 1807539-02-1
  • MF: C18H8F10O5
  • MW: 494.237
  • Catalog: ADC Linker
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 452.6±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 219.4±23.6 °C

Tubulysin IM-2

Tubulysin IM-2 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins.

  • CAS Number: 1032072-50-6
  • MF: C26H42N4O6S
  • MW: 538.70
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG2-acid

Mal-PEG2-acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Mal-PEG2-acid can be conjugated to Tubulysin (HY-128914) and its derivative cytotoxic molecule[1].

  • CAS Number: 1374666-32-6
  • MF: C11H15NO6
  • MW: 257.240
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 455.7±35.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 229.4±25.9 °C

Zuvotolimod

Zuvotolimod is a myeloid cell agonist compound-linker for antibody conjugate. Zuvotolimod can be used in the research of cancer and hepatitis[1][2].

  • CAS Number: 2355262-97-2
  • MF: C55H70N12O10
  • MW: 1059.22
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Duocarmycin MB

Duocarmycin MB is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MB can be used against multi-drug resistant cell lines.

  • CAS Number: 1613286-58-0
  • MF: C27H26ClN3O4
  • MW: 491.97
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Boc-PEG7-alcohol

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

  • CAS Number: 1292268-13-3
  • MF: C19H39NO9
  • MW: 425.514
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 521.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 269.0±30.1 °C

Fmoc-Gly-NH-CH2-O-CH2COOH

Fmoc-Gly-NH-CH2-O-CH2COOH is an ADC linker. Fmoc-Gly-NH-CH2-O-CH2COOH can be used for synthesis of ADCs[1].

  • CAS Number: 1599440-08-0
  • MF: C20H20N2O6
  • MW: 384.38
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Duocarmycin MA

Duocarmycin MA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MA can be used against multi-drug resistant cell lines.

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A