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

DSS Crosslinker

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

  • CAS Number: 68528-80-3
  • MF: C16H20N2O8
  • MW: 368.339
  • Catalog: ADC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 513.5±60.0 °C at 760 mmHg
  • Melting Point: 169-170ºC
  • Flash Point: 264.4±32.9 °C

MMAF-OMe

MMAF-Ome belongs to ADC, and inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4-) cell lines, respectively.

  • CAS Number: 863971-12-4
  • MF: C40H67N5O8
  • MW: 745.989
  • Catalog: ADC Cytotoxin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 871.8±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 481.0±34.3 °C

SCO-PEG7-Maleimide

SCO-PEG7-Maleimide is a cleavable ADC Linker containing 3 PEG units. SCO-PEG7-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: 2143968-81-2
  • MF: C32H51N3O12
  • MW: 669.76
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(2R,3R)Methyl-2-(N-((2S,3R)-3-((9S)-9-((S)-2-((((9H-Fluoren-9-Yl)Methoxy)Carbonyl)(Methyl)Amino)-3-Methylbutanamido)-3-Methoxy-5,10-Dimethyl-4-(Methylamino)-8-Oxoundecanoyl)Pyrrolidin-2-Yl)Propionamido)-3-Methoxy-2-Methyl-3-Phenylpropanoate

Fmoc-MMAF-OMe is an anticancer agent and tubulin polymerization inhibitor with an Fmoc protecting group. The active ingredient of Fmoc-MMAF-OMe, MMAF (HY-15579), is the cytotoxic (ADC Cytotoxin) component of classic antibody drug conjugates (ADCs)[1].

  • CAS Number: 863971-38-4
  • MF: C55H77N5O10
  • MW: 968.23
  • Catalog: ADC Cytotoxin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 1029.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 576.5±34.3 °C

Aminooxy-PEG2-BCN

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

  • CAS Number: 2253965-14-7
  • MF: C19H31N3O6
  • MW: 397.47
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MC-PEG2-NH2

MC-PEG2-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 640267-62-5
  • MF: C16H27N3O5
  • MW: 341.40
  • 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

MC-Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH

MC-Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1599440-25-1
  • MF: C28H36N6O10
  • MW: 616.62
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-NH-ethyl-SS-propionic acid

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

  • CAS Number: 485800-27-9
  • MF: C10H19NO4S2
  • MW: 281.39
  • 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

DMEA-PNU-159682 dichloroacetate

DMEA-PNU-159682 (molecule D12) dichloroacetate is an ADC cytotoxin molecule including metabolites of nemorubicin (MMDX) from liver microsomes and a potent ADCs cytotoxin PNU-159682[1][2].

  • CAS Number: 1799421-49-0
  • MF: C41H49Cl4N3O18
  • MW: 1013.65
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-benzyloxycarbonylazetidine-3-carboxylic acid

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

  • CAS Number: 97628-92-7
  • MF: C12H13NO4
  • MW: 235.236
  • Catalog: ADC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 421.2±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 208.5±28.7 °C

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

Glu(OtBu)-Val-Cit-PAB-OH

Glu(OtBu)-Val-Cit-PAB-OH (compound L5-1c) is an non-cleavable ADC linker. Glu(OtBu)-Val-Cit-PAB-OH has been used to synthesis protein-tubulysin conjugates[1].

  • CAS Number: 2757059-05-3
  • MF: C27H44N6O7
  • MW: 564.67
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

m-PEG12-amine

m-PEG12-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. m-PEG12-amine is also a non-cleavable 12 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 1977493-48-3
  • MF: C25H53NO12
  • MW: 559.688
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 583.6±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 291.3±22.4 °C

Aminooxy-PEG3-azide

Aminooxy-PEG3-azide is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Aminooxy-C2-PEG3-azide is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].

  • CAS Number: 1306615-51-9
  • MF: C8H18N4O4
  • MW: 234.25300
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Diacetyl Agrochelin

Diacetyl Agrochelin is an acetyl derivative of Agrochelin, which is produced by the fermentation of a marine Agrobacterium sp. Diacetyl Agrochelin has cytotoxic activity in tumor cell lines[1].

  • CAS Number: 247115-75-9
  • MF: C27H38N2O6S2
  • MW: 550.73
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

Mc-MMAE

Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate (ADC).

  • CAS Number: 863971-24-8
  • MF: C49H78N6O10
  • MW: 911.17800
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: 1.144±0.06 g/cm3(Predicted)
  • Boiling Point: 1025.2±65.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

β-D-glucuronide-pNP-carbonate

β-D-glucuronide-pNP-carbonate is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 894095-98-8
  • MF: C45H43N3O18
  • MW: 913.83
  • 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

BDP FL DBCO

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

  • CAS Number: 2093197-94-3
  • MF: C32H29BF2N4O2
  • MW: 550.41
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulysin IM-3

Tubulysin IM-3 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins.

  • CAS Number: 1639986-05-2
  • MF: C14H21NO2
  • MW: 235.32
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG2-C2-amine

Azido-PEG2-C2-amine (N3-PEG2-CH2CH2NH2) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Azido-PEG2-C2-amine is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 166388-57-4
  • MF: C6H14N4O2
  • MW: 174.20100
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-NH-ethyl-SS-propionic acid

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

  • CAS Number: 864235-83-6
  • MF: C20H21NO4S2
  • MW: 403.52
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Boc-N-bis(PEG4-OH)

N-Boc-N-bis(PEG4-OH) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2093154-01-7
  • MF: C21H43NO10
  • MW: 469.57
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A