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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Mal-L-PA-NH-Boc

Mal-L-PA-NH-Boc is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 1491152-23-8
  • MF: C12H16N2O6
  • MW: 284.27
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SCO-PEG2-NH2

SCO-PEG2-NH2 is a cleavable ADC Linker containing 2 PEG units. SCO-PEG2-NH2 can be used as a copper-free click chemical reagent for catalyst-free click reactions.

  • CAS Number: 2141976-34-1
  • MF: C15H26N2O4
  • MW: 298.38
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ansamitocin P-3

Ansamitocin P 3' exhibits antitumour activity, is an antibody drug conjugate cytotoxin. The more information please refer to Ansamitocin P-3 (HY-15739).

  • CAS Number: 66547-09-9
  • MF: C32H43ClN2O9
  • MW: 635.145
  • Catalog: ADC Cytotoxin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 833.1±65.0 °C at 760 mmHg
  • Melting Point: 182-185℃
  • Flash Point: 457.7±34.3 °C

Boc-Aminooxy-PEG2-bromide

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

  • CAS Number: 252378-67-9
  • MF: C11H22BrNO5
  • MW: 328.20
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-aminooxy-amide-PEG4-propargyl

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

  • CAS Number: 2253965-01-2
  • MF: C18H32N2O8
  • MW: 404.46
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6-Oxohexanoic acid

6-Oxohexanoic acid is a non-cleavable modified MMAF-C5-COOH linker and can be used in the synthesis of modified MMAF-C5-COOH, a drug-linker conjugate for ADC[1].

  • CAS Number: 928-81-4
  • MF: C6H10O3
  • MW: 130.14200
  • Catalog: ADC Linker
  • Density: 1.088g/cm3
  • Boiling Point: 263.7ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 127.5ºC

PF-06380101

PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and N87 cell line) [1]Target: ADCs cytotoxin; tubulin inhibitorAfter an IV dose of 20a at 20 μg/kg to Wistar Han rats, PF-06380101 exhibited a mean systemic clearance (Cl) of 70 mL/min/kg and a volume of distribution (Vss) of 14.70 L/kg, resulting in a terminal elimination half-life (t1/2) of approximately 6 h. PF-06380101 preferentially distributes into human plasma relative to whole blood and that PF-06380101 is a P-glycoprotein (P-gp) substrate. PF-06380101 is anticipated to be of low risk to perpetrate pharmacokinetic drug interactions with compounds for which CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and/or CYP3A4/5-mediated metabolism constitutes the primary mechanism of clearance. The utility of the new auristatin analogues as ADC payloads including the development of the lead analogue 20a (PF-06380101) will be reported in due course.

  • CAS Number: 1436391-86-4
  • MF: C39H62N6O6S
  • MW: 743.011
  • Catalog: ADC Cytotoxin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 903.1±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 500.0±34.3 °C

BCN-exo-PEG2-NH2

BCN-exo-PEG2-NH2 is an ADC Linker containing 2 PEG units. BCN-exo-PEG2-NH2 contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, BCN reacts with molecules containing azide groups to form stable triazoles in the absence of catalysts.

  • CAS Number: 1357379-13-5
  • MF: C17H28N2O4
  • MW: 324.42
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

22-(tert-Butoxy)-22-oxodocosanoic acid

22-(tert-Butoxy)-22-oxodocosanoic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 22-(tert-Butoxy)-22-oxodocosanoic acid is also a alkyl chain-based PROTAC linker that can be used in t

  • CAS Number: 1642333-05-8
  • MF: C26H50O4
  • MW: 426.673
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMAC-SPP

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

  • CAS Number: 663599-10-8
  • MF: C17H21N3O5S2
  • MW: 411.50
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PC-Biotin-PEG4-PEG3-azide

PC-Biotin-PEG4-PEG3-azide is a cleavable 7 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2055198-04-2
  • MF: C39H63N9O14S
  • MW: 914.03
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-Phe-Lys(Trt)-PAB-PNP

Fmoc-Phe-Lys(Trt)-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1116086-09-9
  • MF: C63H57N5O9
  • MW: 1028.15
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mc-​Val-​Ala-​PAB

Mc-​Val-​Ala-​PAB is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1870916-87-2
  • MF: C25H34N4O6
  • MW: 486.56
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

17-GMB-APA-GA

17-GMB-APA-GA is an ADC Cytotoxin. 17-GMB-APA-GA is a potent HSP90 inhibitor and used for latent T. gondii infection research[1].

  • CAS Number: 256337-10-7
  • MF: C39H53N5O11
  • MW: 767.87
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ALD-PEG4-OPFP

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

  • CAS Number: 1324007-10-4
  • MF: C25H26F5NO8
  • MW: 563.47
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG1-acid

Mal-PEG1-acid is a non-cleavable (1 unit PEG) ADC linker used in the synthesis of antibody-drug conjugates (ADCs)

  • CAS Number: 760952-64-5
  • MF: C9H11NO5
  • MW: 213.187
  • Catalog: ADC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 419.4±30.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 207.5±24.6 °C

Daun02

Daun02 is a prodrug of the topoisomerase inhibitor Daunorubicin.

  • CAS Number: 290304-24-4
  • MF: C41H44N2O20
  • MW: 884.78900
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-NH-PEG4-CH2CH2COOH

Fmoc-NH-PEG4-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 557756-85-1
  • MF: C26H33NO8
  • MW: 487.54200
  • Catalog: ADC Linker
  • Density: 1.219
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-3VVD-OH

Fmoc-3VVD-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 863971-44-2
  • MF: C36H51N3O7
  • MW: 637.80604
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Val-Cit-PABC-Ahx-May

Val-Cit-PABC-Ahx-May is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2126749-74-2
  • MF: C57H82ClN9O15
  • MW: 1168.77
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Upifitamab rilsodotin

Upifitamab rilsodotin (XMT-1536) is an antibody-drug conjugate targeting NaPi2b. Upifitamab rilsodotin can be used for the research of cancer, including Ovarian cancer[1][2].

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

PC Biotin-PEG3-azide

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

  • CAS Number: 1937270-46-6
  • MF: C35H55N9O12S
  • MW: 825.93
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG4-alcohol

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

  • CAS Number: 86770-74-3
  • MF: C8H19NO4
  • MW: 193.241
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 301.6±27.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 136.2±23.7 °C

Tr-PEG5-OH

Tr-PEG5-OH is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 141282-24-8
  • MF: C29H36O6
  • MW: 480.59300
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG3-C1-NHS ester

Mal-PEG3-C1-NHS ester is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2230016-26-7
  • MF: C16H20N2O9
  • MW: 384.34
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Exatecan mesylate

Exatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research[1][2][3].

  • CAS Number: 197720-53-9
  • MF: C24H22FN3O4S.CH4O3S.2H2O
  • MW: 567.58
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1,6-Bis(mesyloxy)hexane

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

  • CAS Number: 4239-24-1
  • MF: C8H18O6S2
  • MW: 274.35500
  • Catalog: ADC Linker
  • Density: 1.273g/cm3
  • Boiling Point: 474.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 240.8ºC

NH2-PEG4-CH2CH2COOH

NH2-PEG4-CH2CH2COOH is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 663921-15-1
  • MF: C11H23NO6
  • MW: 265.303
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 409.6±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 201.5±27.3 °C

Sulfo-DMAC-SPP

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

  • CAS Number: 663599-11-9
  • MF: C17H21N3O8S3
  • MW: 491.56
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Val-Cit-PABC-Ahx-May TFA

Val-Cit-PABC-Ahx-May TFA is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2126749-75-3
  • MF: C59H83ClF3N9O17
  • MW: 1282.79
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A