Signaling Pathways
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.
Products for Signaling Pathways
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- Cat.No. Product Name Information
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GN10814
Quercitrin
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GN10812
Acacetin
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GN10810
Cordycepin
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GN10809
Tanshinone IIA sulfonate sodium
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GN10805
Protopanaxdiol
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GN10804
Isovitexin
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GN10802
Brazilin
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GN10801
Senkyunolide I
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GN10800
20(S)-NotoginsenosideR2
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GN10799
Ginsenoside Rg3
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GN10797
Tangeretin
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GN10792
Caffeic acid
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GN10791
Catharanthine
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GN10788
Cucurbitacin IIb
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GN10784
Rhoifolin
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GN10783
(R) Ginsenoside Rh2
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GN10782
Genistin
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GN10780
Cephalomannine
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GN10779
Reserpine
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GN10778
Picroside II
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GN10776
Obacunone
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GN10768
Leonurine hydrochloride
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GN10764
Homovanillic acid
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GN10762
Gypenoside XLIX
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GN10759
Sanggenone C
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GN10752
Pachymic acid
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GN10751
Dictamnine
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GN10747
Lannaconitine
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GN10745
(+)-Bicuculline
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GN10742
Homoharringtonine
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GN10741
Garcinone D
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GN10740
Tetrahydropalmatine
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GN10737
Tanshinone IIA
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GN10734
Polyphyllin B
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GN10733
Carnosic acid
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GN10732
Oroxin B
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GN10727
Forsythoside B
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GN10720
Gentiopicrin
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GN10718
Andrographolide
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GN10717
Sanguinarine
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GN10716
Epiberberine
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GN10715
Catharanthine Tartrate
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GN10709
Polyphyllin A
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GN10706
Diosimin
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GN10705
Alantolactone
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GN10702
Asiatic acid
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GN10698
Cynarin
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GN10697
Dehydroandrographolide
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GN10696
Garcinone C
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GN10695
Notoginsenoside R1
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GN10693
Rutin
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GN10692
Oridonin
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GN10686
Ginsenoside Rh2
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GN10685
Anemarsaponin B
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GN10683
Tanshinone I
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GN10681
Sophocarpine
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GN10680
Puerarin
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GN10678
Cinnamyl alcohol
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GN10676
Palmitic acid
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GN10673
Liquiritigenin
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GN10669
Glucosamine sulfate
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GN10668
Coenzyme Q10
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GN10667
Calycosin
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GN10666
Isoalantolactone
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GN10664
Honokiol
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GN10663
Coumarin
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GN10662
Cichoric Acid
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GN10654
(+)-Corynoline
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GN10652
Norisoboldine
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GN10650
Ziyuglycoside II
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GN10649
Polygalaxanthone III
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GN10648
Rosmarinic acid
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GN10647
Artemisinine
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GN10646
Engeletin
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GN10645
Jaceosidin
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GN10639
Methyl protodioscin
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GN10638
Artemether
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GN10634
Myricetin
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GN10633
Scutellarein
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GN10632
Betulin
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GN10629
5,7-dihydroxychromone
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GN10627
Atractylenolide I
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GN10625
7-Epitaxol
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GN10624
Scutellarin
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GN10623
Cholic acid
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GN10622
Shikimic acid
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GN10618
Biochanin A
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GN10616
Timosaponin A3
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GN10614
Ginsenoside Rg2
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GN10613
Hesperidin
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GN10612
(+)- Praeruptorin C
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GN10609
Coptisine Sulfate
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GN10607
Nuciferine
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GN10605
(+)-Catechin hydrate
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GN10603
Sennoside B
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GN10599
Procyanidin B2
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GN10592
Platycodin D
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GN10590
Bakuchiol
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GN10585
Tetramethylpyrazine
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GN10584
Ginsenoside Rk1