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.


Anti-infection >
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NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT

NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) is a topoisomerase I inhibitor, which can be delivered to cells through conjugated antibody targeting, and has good ADC activity in vivo and in vitro[1].

  • CAS Number: 2857037-69-3
  • MF: C26H23N3O6
  • MW: 473.48
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Clezutoclax

Clezutoclax is a potent payload and also a Bcl-XL inhibitor. Clezutoclax can be used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1949843-71-3
  • MF: C83H102N12O24S2
  • MW: 1715.89
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

UAA crosslinker 1 hydrochloride

UAA crosslinker 1 hydrochloride is an amber codon used for non-canonical amino acids (ncAAs) incorporation. The ncAAs can be incorporated into proteins in vivo by making use of the promiscuous activity of certain wildtype and engineered aminoacyl-tRNA synthetases[1].

  • CAS Number: 1994331-17-7
  • MF: C9H18ClN5O4
  • MW: 295.72
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Maleimidovaleric acid

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

  • CAS Number: 57078-99-6
  • MF: C9H11NO4
  • MW: 197.188
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 400.7±28.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 196.2±24.0 °C

Sandramycin

Sandramycin ia a cyclic depsipeptide antibiotic isolated from cultured broth of a Nocardioides sp. Sandramycin is also a DNA intercalator that potently binds DNA and is an ADC cytotoxin. Sandramycin is active against Gram-positive bacteria and has potent antitumor activity[1][2][3].

  • CAS Number: 100940-65-6
  • MF: C60H76N12O16
  • MW: 1221.32000
  • Catalog: Bacterial
  • Density: 1.42g/cm3
  • Boiling Point: 1518.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 872.1ºC

SCO-PEG2-Maleimide

SCO-PEG2-Maleimide is an ADC Linker containing 3 PEG units. SCO-PEG2-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: 2141976-23-8
  • MF: C22H31N3O7
  • MW: 449.5
  • Catalog: ADC Linker
  • Density: 1.26±0.1 g/cm3(Predicted)
  • Boiling Point: 693.4±55.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG6-alcohol

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

  • CAS Number: 86770-69-6
  • MF: C12H25N3O6
  • MW: 307.34300
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Butanoyl-L-homoserine lactone

N-Butanoyl-L-homoserine lactone is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N-Butanoyl-L-homoserine lactone has antibacterial activity and is used in antibacterial biofilm[1].

  • CAS Number: 67605-85-0
  • MF: C8H13NO3
  • MW: 171.194
  • Catalog: Bacterial
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 428.1±34.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 212.7±25.7 °C

N3-PEG3-CH2CH2-Boc

N3-PEG3-CH2CH2-Boc is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. N3-PEG3-CH2CH2-Boc is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[2].

  • CAS Number: 252881-73-5
  • MF: C13H25N3O5
  • MW: 303.35500
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-Cystamine

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

  • CAS Number: 485800-26-8
  • MF: C9H20N2O2S2
  • MW: 252.40
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(Iodoacetamido)-Doxorubicin

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

  • CAS Number: 114390-30-6
  • MF: C29H30INO12
  • MW: 711.45
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BCN-exo-PEG2-maleimide

BCN-exo-PEG2-maleimide is an ADC Linker containing 2 PEG units. BCN-exo-PEG2-maleimide contains the lyophilic bidentate macrocyclic ligand BCN, which allows for further synthesis of macrocyclic complexes. In click chemistry, BCN reacts with molecules containing azide groups to form stable triazoles in the absence of catalysts. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.

  • CAS Number: 2141976-22-7
  • MF: C24H33N3O7
  • MW: 475.53
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PC Biotin-PEG3-NHS ester

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

  • CAS Number: 2353409-93-3
  • MF: C36H52N6O15S
  • MW: 840.89
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Doxorubicin hydrochloride

Doxorubicin is a cytotoxic anthracycline antibiotic for the treatment of multiple cancers. The possible mechanisms by which doxorubicin acts in the cancer cell are intercalation into DNA and disruption of topoisomerase-II-mediated DNA repair.

  • CAS Number: 23214-92-8
  • MF: C27H29NO11
  • MW: 543.52
  • Catalog: Bacterial
  • Density: 1.61 g/cm3
  • Boiling Point: N/A
  • Melting Point: 205ºC
  • Flash Point: 443.8ºC

Fmoc-NH-PEG1-CH2COOH

Fmoc-NH-PEG1-CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 260367-12-2
  • MF: C19H19NO5
  • MW: 341.358
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 563.8±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 294.8±30.1 °C

Azido-SS-PEG2-acid

Azido-C2-SS-PEG2-C2-acid is a cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2144777-72-8
  • MF: C9H17N3O4S2
  • MW: 295.38
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-Val-Ala-PAB-PNP

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

  • CAS Number: 1394238-92-6
  • MF: C37H36N4O9
  • MW: 680.70
  • Catalog: ADC Linker
  • Density: 1.322±0.06 g/cm3(Predicted)
  • Boiling Point: 931.4±65.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

H-Glu-OtBu

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

  • CAS Number: 45120-30-7
  • MF: C9H17NO4
  • MW: 203.236
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 326.8±32.0 °C at 760 mmHg
  • Melting Point: 140ºC
  • Flash Point: 151.5±25.1 °C

DBCO-Amine

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

  • CAS Number: 1255942-06-3
  • MF: C18H16N2O
  • MW: 276.33200
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

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-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

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

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

DC4SMe

DC4SMe, a phosphate prodrug of cytotoxic DNA alkylator DC4, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4SMe exhibits IC50s of 1.9 nM, 2.9 nM, and 1.8 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC4SMe can be used for the targeted treatment of cancer[1].

  • CAS Number: 615538-47-1
  • MF: C35H31ClN5O7PS2
  • MW: 764.21
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

rel-2, 5-Dioxopyrrolidin-1-yl 1-((1R, 8S, 9s)-bicyclo[6.1.0]non-4-yn-9-yl)-3-oxo-2, 7, 10, 13, 16-pentaoxa-4-azanonadecan-19-oate

BCN-endo-PEG4-NHS is an ADC Linker containing 4 PEG units. BCN-endo-PEG4-NHS contains the lyophilic bidentate macrocyclic ligand endo-BCN, which allows for further synthesis of 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: 1702356-19-1
  • MF: C26H38N2O10
  • MW: 538.59
  • Catalog: ADC Linker
  • Density: 1.28±0.1 g/cm3(Predicted)
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

polyketomycin

Polyketomycin is a tetracyclic quinone glycoside antibiotic isolated from Streptomyces sp. or Streptomyces diastatochromogenes. Polyketomycin inhibits growth of Gram-positive bacteria, and its MIC values is less than 0.2 µg/mL. Polyketomycin has antibacterial, anticancer, antimalarial activities[1][2][3].

  • CAS Number: 200625-47-4
  • MF: C44H48O18
  • MW: 864.84100
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Glucocorticoid receptor agonist-1 Ala-Ala-Mal

Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88) is a glucocorticosteroid, and an agonist of glucocorticoid receptor. Glucocorticoid receptor agonist-1 Ala-Ala-Mal can be conjugated with Adalimumab (HY-P9908) to prepare an ADC[1].

  • CAS Number: 2166376-51-6
  • MF: C48H54N4O11
  • MW: 862.96
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DC4

DC4, a ADC cytotoxin, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4 can be used for the targeted treatment of cancer[1].

  • CAS Number: 615538-48-2
  • MF: C34H29ClN5O7PS
  • MW: 718.12
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A