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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Paclitaxel

Paclitaxel is a potent anticancer medication which can promote microtubule (MT) assembly, inhibit MT depolymerization, and change MT dynamics required for mitosis and cell proliferation.

  • CAS Number: 33069-62-4
  • MF: C47H51NO14
  • MW: 853.906
  • Catalog: ADC Cytotoxin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 957.1±65.0 °C at 760 mmHg
  • Melting Point: 213 °C (dec.)(lit.)
  • Flash Point: 532.6±34.3 °C

Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br

Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br is an ADC linker that can be used to synthesize ABBV-154, ABBV-927, ABBV-368 or their analogs[1].

  • CAS Number: 2344809-82-9
  • MF: C44H51BrN3O14P
  • MW:
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-tert-Butoxycarbonyl-trans-4-hydroxy-D-proline

N-tert-Butoxycarbonyl-trans-4-hydroxy-D-proline is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N-tert-Butoxycarbonyl-trans-4-hydroxy-D-proline is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].

  • CAS Number: 147266-92-0
  • MF: C10H17NO5
  • MW: 231.246
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 390.9±42.0 °C at 760 mmHg
  • Melting Point: 123ºC
  • Flash Point: 190.2±27.9 °C

diMal-O-CH2COOH

diMal-O-CH2COOH is a cleavable ADC linker.

  • CAS Number: 1620837-47-9
  • MF: C13H12N2O7
  • MW: 308.24
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MC-GGFG-NH-CH2-O-CH2-cyclopropane-COOH

MC-GGFG-NH-CH2-O-CH2-cyclopropane-COOH is an ADC linker that can be combined with the cytotoxic Camptothecin (HY-16560) to form ADC-related drug-linker conjugates (Drug-Linker Conjugates for ADC ).MC-GGFG-NH-CH2-O-CH2-cyclopropane-COOH is conjugated to Camptothecin, which can further bind to the antibody Trastuzumab (HY-P9907) to form Antibody-Drug Conjugates (ADCs)[1].

  • CAS Number: 2778374-70-0
  • MF: C31H40N6O10
  • MW: 656.68
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulysin A

Tubulysin A(TubA) is a myxobacterial product that can function as an antiangiogenic agent in many in vitro assays; anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative.IC50 value: Target: microtubuleTubulysin A is a novel antibiotic, which is anti-microtubule, anti-mitotic, apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative. Tubulysins are cytotoxic peptides, which include 9 members (A-I). Tubulysin A has potential application as an anticancer agent. It arrests cells in the G2/M phase. Tubulysin A inhibits polymerization more efficiently than vinblastine and induces depolymerization of isolated microtubules. Tubulysin A has potent cytostatic effects on various tumor cell lines with IC50 in the picomolar range.

  • CAS Number: 205304-86-5
  • MF: C43H65N5O10S
  • MW: 844.06900
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TCO-GK-PEG4-NHS ester

TCO-GK-PEG4-NHS ester is an ADC Linker, and can be used for synthesis of [18F]AlF-NOTA-Tz-TCO-GK-2Rs15d. [18F]AlF-NOTA-Tz-TCO-GK-2Rs15d binds with high affinity and immunoreactivity to HER2[1].

  • CAS Number: 2307311-19-7
  • MF: C33H52N4O14
  • MW: 728.78
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMAC-SPDB

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

  • CAS Number: 663599-05-1
  • MF: C16H19N3O5S2
  • MW: 397.47
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG3-NHS ester

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

  • CAS Number: 1428629-71-3
  • MF: C14H19NO7
  • MW: 313.303
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 427.2±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 212.1±31.5 °C

β-D-tetraacetylgalactopyranoside-PEG1-N3

β-D-tetraacetylgalactopyranoside-PEG1-N3 is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 153252-36-9
  • MF: C18H27N3O11
  • MW: 461.42
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SG2057

SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent[1].

  • CAS Number: 260417-62-7
  • MF: C33H36N4O6
  • MW: 584.662
  • Catalog: ADC Cytotoxin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 820.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 449.7±34.3 °C

Aldoxorubicin•HCl

Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.

  • CAS Number: 1361563-03-2
  • MF: C37H43ClN4O13
  • MW: 787.21
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMAC-PDB

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

  • CAS Number: 663599-04-0
  • MF: C12H16N2O3S2
  • MW: 300.40
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DBCO-N-bis(PEG4-NHS ester)

DBCO-N-bis(PEG4-NHS ester) is a PEG linker which contains two PEG4-NHS ester and a DBCO group. DBCO-N-bis(PEG4-NHS ester) is useful for protein modification or labeling.

  • CAS Number: 2639395-38-1
  • MF: C49H62N4O18
  • MW: 995.03
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG4-NHS ester

Propargyl-PEG4-NHS ester is a nonclaevable 4-unit PEG linker for antibody-drug-conjugation (ADC).

  • CAS Number: 1428629-70-2
  • MF: C16H23NO8
  • MW: 357.356
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 463.1±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 233.9±31.5 °C

Mal-VC-PAB-PNP

Mal-VC-PAB-PNP is a cleavable ADC Linker (ADC Linker). Mal-VC-PAB-PNP can be used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1096584-62-1
  • MF: C32H37N7O11
  • MW: 695.68
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMAC-SPDB-sulfo

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

  • CAS Number: 663599-07-3
  • MF: C16H19N3O8S3
  • MW: 477.53
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

20-(Tert-Butoxy)-20-Oxoicosanoic Acid

20-(tert-Butoxy)-20-oxoicosanoic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 20-(tert-Butoxy)-20-oxoicosanoic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs

  • CAS Number: 683239-16-9
  • MF: C24H46O4
  • MW: 398.620
  • Catalog: ADC Linker
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 496.0±18.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 152.4±14.7 °C

MAC glucuronide linker-1

MAC glucuronide linker-1 is a nonclaevable ADC linker for antibody-drug-conjugations (ADCs)[1].

  • CAS Number: 2222981-71-5
  • MF: C42H47N3O17S
  • MW: 897.90
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N2'-Deacetyl-N2'-[3-(methyldithio)-1-oxopropyl]maytansine

DM1-SMe is an unconjugated form of the Maytansinoid in IMGN901. DM1-SMe is about 3-10-fold more potent than the parent drug Maytansine, with IC50s ranging from 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines[1].

  • CAS Number: 138148-68-2
  • MF: C36H50ClN3O10S2
  • MW: 784.37900
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG1-SS-alcohol

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

  • CAS Number: 1391914-41-2
  • MF: C7H12O2S2
  • MW: 192.299
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 319.2±32.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 146.8±25.1 °C

Py-MPB-amino-C3-PBD

Py-MPB-amino-C3-PBD is a cytotoxic agent comprised non-alkylating group. Py-MPB-amino-C3-PBD acts as the payload for ADCs. Antimicrobial activity[1].

  • CAS Number: 2412924-07-1
  • MF: C41H44N8O6
  • MW: 744.84
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MMAF (Hydrochloride)

MMAF hydrochloride is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.

  • CAS Number: 1415246-68-2
  • MF: C39H66ClN5O8
  • MW: 768.42300
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Succinic anhydride

Succinic anhydride is a cyclic anhydride and an ADC linker extracted from patent WO2009064913A1. It can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide[1].

  • CAS Number: 108-30-5
  • MF: C4H4O3
  • MW: 100.073
  • Catalog: ADC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 261.0±0.0 °C at 760 mmHg
  • Melting Point: 118-120 °C(lit.)
  • Flash Point: 122.1±15.9 °C

Tetraethylene glycol monotosylate

Tetraethylene glycol monotosylate is a cleavable and acylhydrazone-based ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 77544-60-6
  • MF: C15H24O7S
  • MW: 348.41200
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-Val-Cit-PAB-PNP

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

  • CAS Number: 870487-10-8
  • MF: C30H40N6O10
  • MW: 644.6728
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Aminooxy-PEG4-alcohol

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

  • CAS Number: 106492-60-8
  • MF: C8H19NO5
  • MW: 209.24000
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-Hyp-OMe

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

  • CAS Number: 74844-91-0
  • MF: C11H19NO5
  • MW: 245.272
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 335.2±42.0 °C at 760 mmHg
  • Melting Point: 92-96 °C(lit.)
  • Flash Point: 156.6±27.9 °C

Doxorubicin Hydrochloride

Doxorubicin hydrochloride 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: 25316-40-9
  • MF: C27H30ClNO11
  • MW: 579.980
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: 810.3ºC at 760 mmHg
  • Melting Point: 216ºC
  • Flash Point: 443.8ºC

Tup hydrochloride

Tup hydrochloride is a cleavable ADC linker.

  • CAS Number: 1200041-11-7
  • MF: C12H18ClNO3
  • MW: 259.73
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A