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(40823)

  • GC81566 structure
    GC81566Ro 25-1553 TFA
    Purity: >99.00%

    Ro 25-1553 TFA is a 31 amino acid vasoactive intestinal peptide (VIP) analog, that acts as an agonist for VIP2 receptor ( VPAC2 receptor ).

  • GC81567 structure
    GC81567Ro 25-1553 acetate
    Purity: >98.00%

    Ro 25-1553 acetate is a selective VIP 2 receptor ( VPAC 2 receptor ) agonist.

  • GC81568 structure
    GC81568M464
    Purity: >99.50%

    M464, a non-steroidal anti-inflammatory compound, is a potent and orally active NLRP3 inflammasome inhibitor.

  • GC81569 structure
    GC81569Elfetabart
    CAS: 3061153-83-8
    Purity: >99.00%

    Elfetabart (DB-1311 Antibody; BNT324 Antibody) is a humanized monoclonal antibody targeting CD276 with antitumor activity.

  • GC81570 structure
    GC81570Daxdilimab (FUT8-KO)
    Purity: >97.00%

    Daxdilimab (FUT8-KO) is an anti- ILT7 monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out.

  • GC81571 structure
    GC815713,4,6-Tri-O-galloyl-D-glucose
    CAS: 99523-99-6
    Purity: >98.00%

    3,4,6-Tri-O-galloyl-D-glucose (3,4,6-Trigalloylglucose) is an α-amylase ( porcine α-amylase IC 50 = 334.6 μM; K i = 307.5 μM) and α-glucosidase ( yeast α-glucosidase IC 50 = 46.5 μM; K i = 39.9 μM) mixed type inhibitor.

  • GC81572 structure
    GC81572Glutathione trisulfide TFA
    Purity: >99.00%

    Glutathione trisulfide TFA (GSSSG TFA) is an orally active, blood-brain barrier permeable neuroprotective agent.

  • GC81573 structure
    GC81573Indigoidine
    CAS: 2435-59-8
    Purity: >95.00%

    Indigoidine is a natural biological pigment that appears in a bright blue color and is a natural blue dye with industrial applications.

  • GC81574 structure
    GC81574Hydroxyproline
    CAS: 6912-67-0
    Purity: >98.00%

    Hydroxyproline (DL-Hydroxyproline) is a non-essential amino acid and one of the main components of collagenous tissues.

  • GC81575 structure
    GC81575ZIP14-IN-1
    CAS: 1048-17-5
    Purity: >99.50%

    ZIP 14-IN-1 (PPTD) is a selective and orally active ZIP14 inhibitor.

  • GC81576 structure
    GC81576USF 2550A
    CAS: 5192-62-1
    Purity: >98.00%

    USF 2550A is a class of fungus-derived 2-pyran compound with DPPH free radical scavenging activity.

  • GC81577 structure
    GC81577Mono N-desmethyl disperse polyester dark blue
    CAS: 56524-77-7
    Purity: >98.00%

    Mono N-Desmethyl Disperse Polyester Dark Blue is a bioreductive agent that is activated under hypoxic conditions.

  • GC81578 structure
    GC81578Disperse polyester dark blue
    CAS: 56524-76-6
    Purity: >98.00%

    Disperse Polyester Dark Blue is a chemical compound extensively employed in scientific research.

  • 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: >98.00%

    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: >98.00%

    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.