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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Propargyl-O-C1-amido-PEG3-C2-NHS ester

Propargyl-O-C1-amido-PEG3-C2-NHS ester is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2101206-78-2
  • MF: C18H26N2O9
  • MW: 414.41
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MAC glucuronide linker

MAC glucuronide linker is a linker for antibody-drug-conjugations (ADCs) and is useful to prepare the MAC glucuronide SN-38 drug linker[1].

  • CAS Number: 2260960-07-2
  • MF: C43H48BrN3O17S
  • MW: 990.82
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methyl 1-Cbz-azetidine-3-carboxylate

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

  • CAS Number: 757239-60-4
  • MF: C13H15NO4
  • MW: 249.262
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 414.9±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 204.7±28.7 °C

N-Boc-Val-Dil-Dap-Doe

N-Boc-Val-Dil-Dap-Doe is a compound used to synthesize Dolastatin 10. Dolastatin 10, a potent antimitotic peptide, inhibits tubulin polymerization[1].

  • CAS Number: 135383-62-9
  • MF: C40H63N5O7S
  • MW: 758.02
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Inebilizumab

Inebilizumab is an anti-CD19 monoclonal antibody (mAb) with enhanced antibody-dependent cell-mediated cytotoxicity against B cells. Inebilizumab can be used for multiple sclerosis and neuromyelitis optica research[1].

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

Azido-PEG5-Ala-Ala-Asn-PAB

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

  • CAS Number: 2055048-54-7
  • MF: C30H47N7O12
  • MW: 697.73
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ADC toxin 1

ADC toxin 1 is an ADC cytotoxin with anti-cancer activities. ADC toxin 1 is against  HCT-116 and PSN1 cells growth with both IC50 values of 0.86 µM.

  • CAS Number: 723340-57-6
  • MF: C32H52O9
  • MW: 580.75
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-Val-Cit-PAB

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

  • CAS Number: 870487-09-5
  • MF: C23H37N5O6
  • MW: 479.570
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 771.3±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 420.3±32.9 °C

10-Deacetyl-7-xylosyl paclitaxel

10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative with improved pharmacological features and higher water solubility.IC50 value:Target: Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cycle arrest and apoptosis as measured by flow cytometry, DNA laddering, and transmission electron microscopy. Pro-apoptotic Bax and Bad protein expression was up-regulated and anti-apoptotic Bcl-2 and Bcl-XL expression down-regulated, which lead to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9. In turn, caspase-9 activated downstream caspases-3 and -6, but not caspase-8. Bid was also activated by caspase-3. Reversely, treatment with a caspase-10-specific inhibitor could not protect PC-3 cells from 7-xylosyl-10-deacetyl-paclitaxel-triggered apoptosis. Moreover, 7-xylosyl-10-deacetylpaclitaxel had no effect on the expression of CD95 and NF-kappaB proteins, indicating that apoptosis was induced through the mitochondrial-dependent pathway in PC-3 cells.

  • CAS Number: 90332-63-1
  • MF: C50H57NO17
  • MW: 943.984
  • Catalog: ADC Cytotoxin
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 1068.4±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 599.9±34.3 °C

BCN-exo-PEG7-maleimide

BCN-exo-PEG7-maleimide is an ADC Linker containing 7 PEG units. BCN-exo-PEG7-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: 2143965-47-1
  • MF: C34H53N3O12
  • MW: 695.80
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

mDPR(Boc)-Val-Cit-PAB

mDPR(Boc)-Val-Cit-PAB is a cleavable ADC linker used as a linker for antibody-drug conjugates (ADC)[1].

  • CAS Number: 2281797-55-3
  • MF: C30H43N7O9
  • MW: 645.70
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-Val-Cit-OH

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

  • CAS Number: 870487-08-4
  • MF: C16H30N4O6
  • MW: 374.433
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 624.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 331.7±31.5 °C

Exatecan-methylacetamide-OH

Exatecan-methylacetamide-OH (compound 6) is a Exatecan derivative with anticancer effects. Exatecan-methylacetamide-OH is an ADC cytotoxin that can be used to synthesize Antibody-Drug Conjugates (ADCs) (CN112125915A; compound 6)[1].

  • CAS Number: 2594423-51-3
  • MF: C27H26FN3O6
  • MW: 507.51
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG5-C2-acid

Amino-PEG5-C2-acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1191078-74-6
  • MF: C13H27NO7
  • MW: 309.356
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 446.0±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 223.5±28.7 °C

Val-Lys(Boc)-PAB

Val-Lys(Boc)-PAB is a ADC linker. Val-Lys(Boc)-PAB was used to prepare camptothecin peptide conjugates as antitumor agents (WO 2019195665). It was used as a non-​linear self-​immolative linker for reducing hydrophobicity of antibody-​drug conjugates for cancer therapy (WO 2018069375).

  • CAS Number: 1432969-86-2
  • MF: C23H38N4O5
  • MW: 450.58
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

THP-SS-PEG1-Tos

THP-SS-PEG1-Tos is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1807512-37-3
  • MF: C16H24O5S3
  • MW: 392.554
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 539.4±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 280.0±30.1 °C

6-O-2-Propyn-1-yl-D-galactose

6-O-2-Propyn-1-yl-D-galactose is a glycolinker for the functionalization of cytotoxic drugs and applications in antibody-drug conjugation.

  • CAS Number: 881895-59-6
  • MF: C9H14O6
  • MW: 218.20
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-Val-Cit-PAB-OH

Fmoc-Val-Cit-PAB is a linker for antibody-drug-conjugation (ADC).

  • CAS Number: 159858-22-7
  • MF: C33H39N5O6
  • MW: 601.69300
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH2-methylpropanamide-Exatecan TFA

NH2-methylpropanamide-Exatecan TFA is a methylpropanamide-modified Exatecan (HY-13631), which is the common ADC Cytotoxin used in the synthesis of ADC. Exatecan 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].

  • CAS Number: 1817857-35-4
  • MF: C30H30F4N4O7
  • MW: 634.58
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Exatecan (Mesylate)

Exatecan Mesylate is a water soluble topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.

  • CAS Number: 169869-90-3
  • MF: C25H26FN3O7S
  • MW: 531.55300
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-Asp-NH2

Fmoc-Asp-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 200335-40-6
  • MF: C19H18N2O5
  • MW: 354.35700
  • Catalog: ADC Linker
  • Density: 1.362g/cm3
  • Boiling Point: 662.1ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 354.2ºC

Luisol A

Luisol A, an aromatic tetraol, is a major metabolite of an estuarine marine actinomycete of the genus Streptomyces. Luisol A, anthraquinone antibiotic analog, is an ADC Cytotoxin[1].

  • CAS Number: 225110-59-8
  • MF: C16H18O7
  • MW: 322.310
  • Catalog: ADC Cytotoxin
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 587.2±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 221.4±23.6 °C

MC-Val-Cit-PAB-Indibulin

MC-Val-Cit-PAB-indibulin has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-indibulin is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].

  • CAS Number: 2055896-95-0
  • MF: C50H55ClN9O8
  • MW: 945.48
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-C4-amide-C5-NH2

Biotin-C4-amide-C5-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 151294-96-1
  • MF: C14H26N4O2S
  • MW: 314.447
  • Catalog: ADC Linker
  • Density: 1.1±0.0 g/cm3
  • Boiling Point: 650.1±0.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 347.0±0.0 °C

OH-Glu-Val-Cit-PAB-MMAE

OH-Glu-Val-Cit-PAB-MMAE consists a cleavable ADC linker (OH-Glu-Val-Cit-PAB) and a potent tubulin inhibitor (MMAE). SuO-Glu-Val-Cit-PAB-MMAE can be used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1895916-23-0
  • MF: C63H100N10O15
  • MW: 1237.53
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG6-acid

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

  • CAS Number: 1951438-84-8
  • MF: C16H28O8
  • MW: 348.389
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 462.8±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 157.6±22.2 °C

Fmoc-PEG4-Ala-Ala-Asn-PAB

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

  • CAS Number: 2055048-57-0
  • MF: C43H55N5O13
  • MW: 849.92
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-Gly-PEG3-endo-BCN

Boc-gly-PEG3-endo-BCN is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Boc-gly-PEG3-endo-BCN is also a cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 2110444-63-6
  • MF: C28H47N3O8
  • MW: 553.69
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ansamitocin P-3

Ansamitocin P-3 is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic.

  • CAS Number: 66584-72-3
  • 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: 190-192℃
  • Flash Point: 457.7±34.3 °C

HO-PEG10-CH2CH2COO<sup>t</sup>Bu

Hydroxy-PEG10-Boc is extacted from patent CN108707228 (example 0024)[1]. Hydroxy-PEG10-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG10-Boc can be conjugated to Paclitaxel (HY-B0015) or docetaxel (HY-B0011)[2].

  • CAS Number: 778596-26-2
  • MF: C27H54O13
  • MW: 586.71000
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A