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(40698)

  • GC91841 structure
    GC91841Mca-VDQVDGW-K(Dnp)-NH2 (acetate)
    Purity: >95.00%

    Mca-VDQVDGW-K(Dnp)-NH2 is a substrate for caspase-7.

  • GC91849 structure
    GC91849Autocamtide-2-related Inhibitory Peptide (trifluoroacetate salt)
    Purity: >95.00%

    Autocamtide-2-related inhibitory peptide is a calmodulin-dependent protein kinase II (CaMKII) inhibitor (IC50 = 40 nM) that was designed based on the sequence around the autophosphorylation site (Thr286/Thr287) in the autoinhibitory domain of the protein kinase.

  • GC91851 structure
    GC91851Malantide (trifluoroacetate salt)
    Purity: >98.00%

    Malantide is a synthetic peptide derived from the β-subunit of human phosphorylase kinase and is a fluorescent substrate for PKA and PKC.

  • GC91852 structure
    GC91852NFF-3 (trifluoroacetate salt)
    Purity: >95.00%

    NFF-3 is a fluorogenic substrate of matrix metalloproteinases (MMPs).

  • GC91857 structure
    GC91857Kdo2-Lipid A (sodium salt)

    Kdo2-Lipid A is the active component of LPS.

  • GC91866 structure
    GC91866Apelin-36 (trifluoroacetate salt)
    Purity: >95.00%

    The apelin gene encodes a preproprotein that is processed to generate a variety of bioactive peptides, including those having 36, 17, or 13 amino acids (apelin-36, apelin-17, and apelin-13, respectively).

  • GC91874 structure
    GC91874Polysarcosine20
    Purity: >90.00%

    Polysarcosine20 es un polímero hidrofílico funcioncon aminas.

  • GC91884 structure
    GC91884DSPE-PEG(2000)-Mannose
    CAS: 1829524-73-3
    Purity: >98.00%

    DSPE-PEG(2000)-Mannose se ha utilizado en la generación de liposomas y micelas mixtas para la administración de agentes anticancerosos a los macrófagos asociados a tumores TAMs in vitro e in vivo.

  • GC91887 structure
    GC91887Methyl Salicylate-d4
    CAS: 1219802-12-6
    Purity: >99.00%

    Methyl Salicylate-d4 está destinado a usarse como norma interna para la cuantificación del salicilato de metilo mediante GC- o LC-MS.

  • GC91889 structure
    GC91889L-Tyrosine (sodium salt hydrate)
    Purity: >98.00%

    L-Tyrosine (sodium salt hydrate) es un aminoácido condiesencial.

  • GC91898 structure
    GC91898BI SF3 (hydrochloride)
    CAS: 1801257-24-8
    Purity: >95.00%

    BI SF3 (hydrochloride) es un intermediario sintético.

  • GC91899 structure
    GC91899Carmustine-d8
    Purity: >99.00%

    Carmustine-d8 está destinado a usarse como norma interna para la cuantificación de carmustina por GC- o LC-MS.

  • GC91904 structure
    GC91904CNBSF
    CAS: 3829-23-0

    CNBSF es un inhibiirreversible de la glutatión s-transferasa − 1-1 (GSTP1-1) y GST − 1-1 (GSTA1; IC50s = 21 y 1.4 μM, respectivamente).

  • GC91906 structure
    GC91906(R)-AS-1
    CAS: 2506367-95-7
    Purity: >95.00%

    (R)-AS-1 es un modulador alostérico positivo del transportador de aminoácidos excitatorio 2 EAAT2; EC50 = 11 nM en un ensayo de absorción de glutam.

  • GC91909 structure
    GC91909Fenoprofen-13C6 (sodium salt hydrate)
    CAS: 2687960-29-6
    Purity: >98.00%

    Fenoprofen-13C6 (sodium salt hydrate) está diseñado para usarse como un estándar interno para la cuantificación de fenoprofeno por GC- o LC-MS.

  • GC91910 structure
    GC91910Ferroptosis Inhibitor D1
    Purity: >98.00%

    Ferroptosis Inhibitor D1 es un eliminador de radicales libres y un inhibide la ferroptosis.

  • GC91911 structure
    GC91911Napirimus
    CAS: 70696-66-1
    Purity: >95.00%

    Napirimus es un inmunosupres.

  • GC91913 structure
    GC91913NS 3861
    CAS: 216853-59-7
    Purity: >98.00%

    NS 3861 es un agonista del receptor nicotínico acetilcolina (nAChR).

  • GC91914 structure
    GC91914MSH Release-Inhibiting Factor (trifluoroacetate salt)
    Purity: >95.00%

    MSH Release-Inhibiting Factor (trifluoroacetate salt) (MSH-R-IF) es un tripéptido hipotalámico que se une al estride de rata (Kd = 4,69 nM) y tiene diversas actividades biológicas.

  • GC91915 structure
    GC91915ZG-2033
    CAS: 2685739-28-8
    Purity: >98.00%

    ZG-2033 es un agonista del factor inducible por hipoxia 2α (HIF-2α).

  • GC91919 structure
    GC91919Pro-GA
    CAS: 2222067-12-9

    Pro-GA es una forma profarmacológica de n-glutaril-l-alanina y un inhibide la − -glutamilciclotransferasa (GGCT), una enzima involucrada en el metabolismo del glutatión.

  • GC91920 structure
    GC91920Rhein-13C6
    Purity: >95.00%

    Rhein-13C6 está destinado a usarse como norma interna para la cuantificación de Rhein por GC- o LC-MS.

  • GC91921 structure
    GC91921Fenclofenac
    CAS: 34645-84-6
    Purity: >95.00%

    Fenclofenac es un antiinflamatorio no esteroide(AINE) y un inhibidor de la COX (IC50s = 7 y 4 μM para COX-1 y COX-2, respectivamente).

  • GC91922 structure
    GC919226,6-Dimethyl-3-(4-methylbenzoyl)-4,5,6,7-tetrahydro-1-benzothiophen-2-amine
    CAS: 1461715-47-8
    Purity: >95.00%

    6,6-Dimethyl-3-(4-methylbenzoyl)-4,5,6,7-tetrahydro-1-benzothiophen-2-amine es un modulador alostérico PAM positivo del receptor GLP-1R.