GLPBio

Signaling Pathways

Research Area, Signaling Pathways | GlpBio Life Science Products Suppliers

Read More about this category

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.

Research Areas

Products Related to Signaling Pathways(39495)

  • GC81579 structure
    GC81579Ophthalmic acid TFA
    Purity: >98.00%

    Ophthalmic acid TFA is a ubiquitous metabolite and glutathione modulator, with a K i of 0.95 mM for glyoxalase I.

  • GC81580 structure
    GC81580MiADMSA
    CAS: 142609-62-9
    Purity: >98%

    MiADMSA (Monoisoamyl meso-2,3-dimercaptosuccinic acid) is an orally active thiol chelator that can effectively remove heavy metals such as arsenic and lead from the body of animals.

  • GC81581 structure
    GC81581Mal-C2-amide-C10-tri-GalNAc
    CAS: 2893765-20-1
    Purity: >99.50%

    Mal-C2-amide-C10-tri-GalNAc is an asialoglycoprotein receptor ( ASGPR ) binding ligand fragment and a component of lysosome-targeted bifunctional molecules.

  • GC81582 structure
    GC81582HTS13286
    CAS: 727359-12-8
    Purity: >98.50%

    HTS13286 is a novel AQP9 inhibitor.

  • GC81583 structure
    GC81583HCM-01
    CAS: 2117631-52-2
    Purity: >99.00%

    HCM-01 is an Excitatory amino acid transporter 2 ( EAAT2 ) activator with oral effectiveness and blood-brain barrier penetration.HCM-01 binds to the allosteric site of EAAT2, increases EAAT2 expression in astrocytes, enhances glutamate-handling capacity, and modulates glutamate homeostasis.HCM-01 acts as an antioxidant, improves oxidative/antioxidative balance and increases total antioxidant capacity.

  • GC81584 structure
    GC815842-Amino-2-deoxy-D-glucopyranose
    CAS: 90-77-7
    Purity: >98.00%

    2-Amino-2-deoxy-D-glucopyranose is an isomeric form of Glucosamine.

  • GC81585 structure
    GC81585Piezo1 agonist 2
    CAS: 3124796-49-9
    Purity: >98%

    Piezo1 agonist 2 (Compound PD2) is a blood-brain barrier-permeable Piezo1 agonist and Jedi2 conjugate that utilizes LAT1.

  • GC81586 structure
    GC81586Anti-ZnT8 Antibody (mAb43)
    Purity: >99.00%

    Anti-ZnT8 Antibody (mAb43) is a monoclonal antibody targeting the zinc transporter ZnT8, with islet-specific biodistribution characteristics.

  • GC81587 structure
    GC81587Atidafonat
    CAS: 1628848-73-6
    Purity: >99.00%

    Atidafonat is an orally active sodium-dependent phosphate transporter inhibitor, with IC 50 values of 6.8, 1.5, and 1.7 μM against human NaPi-IIb, PiT-1, PiT-2, respectively; and IC 50 values of 3.9, 1.9, and 1.7 μM against rat NaPi-IIb, PiT-1, PiT-2, respectively.

  • GC81588 structure
    GC81588LP-911888
    Purity: >99.50%

    LP-911888 is an orally active ACSL5/ACSL1 inhibitor, with IC 50 values of 1 nM and 3 nM against mouse and human ACSL5, and IC 50 values of 2 nM and 9 nM against mouse and human ACSL1, respectively.

  • GC81589 structure
    GC81589ACSL5-IN-3
    CAS: 3098298-22-4
    Purity: >99.50%

    ACSL5-IN-3 (page 115 line 11) is an ACSL5 inhibitor.

  • GC81590 structure
    GC81590Onjisaponin R
    CAS: 1008798-85-3
    Purity: >98%

    Onjisaponin R is an α-amylase inhibitor.

  • GC81591 structure
    GC815914,5,6,7-Tetrahydro-1,2-benzoxazole-3-carboxylic acid
    CAS: 90005-77-9
    Purity: >98.00%

    4,5,6,7-Tetrahydro-1,2-benzoxazole-3-carboxylic acid (Compound 244) is an indole compound.

  • GC81592 structure
    GC81592ToP-DNJ
    CAS: 1508303-85-2
    Purity: >98%

    ToP-DNJ is a selective endoplasmic reticulum α-glucosidase II ( GluII ) inhibitor with an IC 50 value of 9.0 μM.

  • GC81593 structure
    GC81593Hepcidin-25 (human) TFA
    Purity: >97.00%

    Hepcidin-25 (human) TFA is an iron metabolism modulator and Antimicrobial agent.

  • GC81594 structure
    GC81594TLSC702
    CAS: 748786-57-4
    Purity: >95.50%

    TLSC702 is a human glyoxalase I ( hGLO I ) inhibitor with an IC 50 of 2.0 μM.

  • GC81595 structure
    GC81595BCS12
    CAS: 329719-71-3
    Purity: >99.50%

    BCS12 is a CAIX inhibitor.

  • GC81596 structure
    GC81596SHMT2-IN-1
    Purity: >99.50%

    SHMT2-IN-1 is a potent serine hydroxymethyltransferase 2 ( SHMT2 ) inhibitor with an IC 50 of 1.21 μM and a K D of 10.6 μM.

  • GC81597 structure
    GC81597Momilactone B
    CAS: 51415-08-8
    Purity: >99.00%

    Momilactone B is an inhibitor of α-amylase and α-glucosidase, with an IC 50 of 146.85 μg/mL against Aspergillus oryzae α-amylase and an IC 50 of 612.03 μg/mL against Saccharomyces cerevisiae α-glucosidase.

  • GC81598 structure
    GC81598Emicizumab (Anti-F9 & Factor IX)
    Purity: >99.50%

    Emicizumab (Anti-F9 & Factor IX) is a bispecific monoclonal antibody that bridges activated factor IX and factor X to replace the function of missing activated factor VIII, thereby restoring hemostasis.

  • GC81600 structure
    GC81600S-D-Lactoylglutathione
    CAS: 41656-56-8
    Purity: >98.50%

    S-D-Lactoylglutathione (S-Lactylglutathione; (R)-S-Lactoylglutathione) is a multifunctional metabolic intermediate of the glyoxalase system.

  • GC81601 structure
    GC816012-Hydroxymelatonin
    CAS: 229018-17-1
    Purity: >98.00%

    2-Hydroxymelatonin is a major hydroxylated metabolite of Melatonin.

  • GC81602 structure
    GC81602Glucosamine sulfate potassium chloride
    CAS: 1296149-08-0
    Purity: >98.00%

    Glucosamine sulfate potassium chloride is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement.

  • GC81603 structure
    GC816034’-Phosphopantetheine
    CAS: 2226-71-3
    Purity: >97.50%

    4’-Phosphopantetheine is an orally active coenzyme A (CoA) precursor.