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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DOTA-​NHS-​ester

DOTA-NHS-ester is a linker for affibody molecules and is applied in small animals PET, SPECT, and CT. DOTA-NHS-ester can be used to label radiotherapeutic agents or imaging probes for the detection of tumors[1].

  • CAS Number: 170908-81-3
  • MF: C20H31N5O10
  • MW: 501.48800
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG2-VCP-Eribulin

Mal-PEG2-VCP-Eribulin consists the ADCs linker (Mal-PEG2-VCP) and Eribulin[1]. Eribulin is a mechanistically unique microtubule inhibitor for cancer[2]. Mal-PEG2-VCP-Eribulin is an Eribulin-based drug for antibody conjugates[1].

  • CAS Number: 2130869-18-8
  • MF: C70H99N7O21
  • MW: 1374.57
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG9-bromide

Propargyl-PEG9-bromide is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2055042-83-4
  • MF: C21H39BrO9
  • MW: 515.43
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG4-Br

Propargyl-PEG4-Br is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1308299-09-3
  • MF: C11H19BrO4
  • MW: 295.170
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 334.3±32.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 135.7±23.6 °C

Amino-PEG2-C2-acid

Amino-PEG2-C2-acid is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 791028-27-8
  • MF: C7H15NO4
  • MW: 177.198
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 331.5±27.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 154.3±23.7 °C

ε-Amanitin

ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II[1][2].

  • CAS Number: 21705-02-2
  • MF: C39H53N9O14S
  • MW: 903.95500
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Maytansinoid B

Maytansinoid B is a kind of ADC Cytotoxin. Maytansinoid B can be used to conjugates with antibodies to form Antibody-Drug Conjugates (ADCs). Maytansinoids are known as antimitotic agents, binding to tubulin and inhibiting microtubule assembly. Maytansinoids induces G2/M arrest in the cell cycle to induce apoptosis[1][2].

  • CAS Number: 1628543-40-7
  • MF: C36H51ClN4O10
  • MW: 735.26
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PC Alkyne-PEG4-NHS ester

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

  • CAS Number: 1802907-98-7
  • MF: C29H39N3O14
  • MW: 653.63
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VCP-Eribulin

VCP-Eribulin consists the ADCs linker (VCP) and Eribulin[1]. Eribulin is a mechanistically unique microtubule inhibitor for cancer[2]. VCP-Eribulin is an Eribulin-based drug for antibody conjugates[1].

  • CAS Number: 2130869-17-7
  • MF: C59H86N6O16
  • MW: 1135.34
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MC-Val-Cit-PAB-rifabutin

MC-Val-Cit-PAB-rifabutin 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-rifabutin 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: 2055900-34-8
  • MF: C74H101N10O17
  • MW: 1402.65
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG10-alcohol

m-PEG10-alcohol (Decaethylene glycol monomethyl ether) is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. m-PEG10-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 27425-92-9
  • MF: C21H44O11
  • MW: 472.568
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 524.3±45.0 °C at 760 mmHg
  • Melting Point: 19ºC
  • Flash Point: 270.9±28.7 °C

AcLys-PABC-VC-Aur0101 intermediate-1

AcLys-PABC-VC-Aur0101 intermediate-1 is a cathepsin cleavable ADC linker that is used for making antibody-drug conjugate[1].

  • CAS Number: 1609108-48-6
  • MF: C41H53N7O8
  • MW: 771.90
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MC-Alkyl-Hydrazine Modified MMAF

MC-AlkyMC-Alkyl-Hydrazine is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1404071-64-2
  • MF: C59H92N10O12
  • MW: 1133.42
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG7-Ms

m-PEG7-Ms is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 477775-57-8
  • MF: C16H34O10S
  • MW: 418.50000
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

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

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

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

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

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

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

Hydroxy-PEG3-(CH2)2-Boc

Hydroxy-PEG2-(CH2)2-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG2-(CH2)2-Boc is extracted from patent WO2004008101A2 (compound 196)[1].

  • CAS Number: 186020-66-6
  • MF: C13H26O6
  • MW: 278.34200
  • Catalog: ADC Linker
  • Density: 1.057g/cm3
  • Boiling Point: 365.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 125.2ºC

DBCO-acid

DBCO-acid is a cleavable ADC linker used in the synthesis of ADC linker DBCO-NHS ester (HY-115524 and HY-115545), and drug-linker conjugates DBCO-PEG-MMAE (HY-111012 and HY-126690)[1].

  • CAS Number: 1353016-70-2
  • MF: C19H15NO3
  • MW: 305.32700
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rebeccamycin

Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II[1][2].

  • CAS Number: 93908-02-2
  • MF: C27H21Cl2N3O7
  • MW: 570.37800
  • Catalog: ADC Cytotoxin
  • Density: 1.87g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mensacarcin

Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs)[1][2].

  • CAS Number: 808750-39-2
  • MF: C21H24O9
  • MW: 420.410
  • Catalog: ADC Cytotoxin
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 656.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 232.9±25.0 °C

Mertansine

Mertansine (DM1) is a microtubulin inhibitor which binds at the tips of microtubules and suppresses the dynamicity of microtubules.. Mertansine is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.

  • CAS Number: 139504-50-0
  • MF: C35H48ClN3O10S
  • MW: 738.288
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: 1.33±0.1 g/cm3
  • Boiling Point: 937.1±65.0 °C at 760 mmHg
  • Melting Point: 190-192 ºC
  • Flash Point: 520.5±34.3 °C

Daunorubicin HCl

Daunorubicin hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities.

  • CAS Number: 23541-50-6
  • MF: C27H30ClNO10
  • MW: 563.981
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: 770ºC at 760 mmHg
  • Melting Point: 188 - 190ºC
  • Flash Point: 419.5ºC

Azido-PEG9-amine

Azido-PEG9-amine is a non-cleavable 9 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 1207714-69-9
  • MF: C20H42N4O9
  • MW: 482.569
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DBCO-NHS ester

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

  • CAS Number: 1353016-71-3
  • MF: C23H18N2O5
  • MW: 402.39900
  • Catalog: ADC Linker
  • Density: 1.43±0.1 g/cm3
  • Boiling Point: 670.2±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: N/A