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 는 아민 관능화의 친수성 중합체이다.

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

    DSPE-PEG(2000)-Mannose 이미 지질체와 혼합접착제를 제조하여 체외와 체내에서 항암제를 종양관련 대식세포 TAM에 전달하는데 사용되였다.

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

    Methyl Salicylate-d4는 GC-또는 LC-MS에 의한 메틸 살리실 레이트의 정량을위한 내부 표준으로 사용하기위한 것입니다.

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

    L-Tyrosine (sodium salt hydrate)는 조건부로 필수 아미노산이다.

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

    BI SF3 (hydrochloride)일종의 합성 중간체이다.

  • GC91899 structure
    GC91899Carmustine-d8
    Purity: >99.00%

    Carmustine-d8 는 기상 크로마토그래프 또는 액상 크로마토그래프-질량 크로마토그래프 정량 카모스틴의 내표로 사용하기 위한 것이다.

  • GC91904 structure
    GC91904CNBSF
    CAS: 3829-23-0

    CNBSF은 되돌 릴 수 없는 억제 제야의 글 루타 티 온 S-transferase π 1-1 (GSTP1-1)와하 α 1-1 (GSTA1;IC50s = 21. 4 μ M, 각각)다.

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

    (R)-AS-1 는 흥분성 아미노산 트랜스퍼 단백질 2 EAAT2의 양변조 조절제입니다.글루타민산 섭취 시험에서의 EC50=11nM.

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

    Fenoprofen-13C6 (sodium salt hydrate) GC 또는 LC-MS를 통해 비노로핀을 정량하는 내표로 사용하도록 설계되었습니다.

  • GC91910 structure
    GC91910Ferroptosis Inhibitor D1
    Purity: >98.00%

    Ferroptosis Inhibitor D1는 자유 라디칼 소거 물질이며 강균증 억제제입니다.

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

    Napirimus는 면역 억제제의 일종이다.

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

    NS 3861 는 뉴런 니코틴형 아세틸콜린 수용체(nAChR) 흥분제다.

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

    MSH Release-Inhibiting Factor (trifluoroacetate salt) (MSH-R-IF)는 rat 선조체 (Kd = 4.69 nM)에 결합하는 시상하부 트리펩타이드이며 다양한 생물학적 활성을 가지고 있다.

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

    ZG-2033 는 산소부족 유도인자 2 α (HIF-2 α) 의 흥분제입니다.

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

    Pro-GA 는 N-펜디옥사이드-L-아미노산의 전약형태이자 감마-글루타메이트환전이효소(GGCT)의 억제제로서 GGCT는 글루타메이트의 대사에 관여하는 효소이다.

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

    Rhein-13C6 GC 또는 LC-MS 정량 대황산의 내표로 사용하도록 설계되었습니다.

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

    Fenclofenac은 비스테로이드 항염증제(NSAID)와 COX 억제제(COX-1과 COX-2의 IC50은 각각 7과 4μM)의 일종이다.

  • 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 는 인슐린 샘플 펩타이드 1 수용체 GLP-1R 양성 변조 조절제 PAM입니다.