GlpBio

Antibody-drug Conjugate/ADC Related

Antibody-drug Conjugate/ADC Related(抗体偶联药物相关)

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.

研究方向

Antibody-drug Conjugate/ADC Related 相关产品(844)

  • GC60627 structure
    GC60627BCN-PEG4-acid
    CAS: 1881221-47-1

    BCN-PEG4-acid是一种可降解(cleavable)的含4个单元PEG的ADClinker，可用于合成抗体偶联药物(ADC)。

  • GC60651 structure
    GC60651Boc-Dap-NE
    CAS: 160800-65-7

    Boc-Dap-NE是一种二肽，用作一种可降解(cleavable)的ADClinker，可用于合成抗体偶联药物(ADC)。

  • GC60655 structure
    GC60655Boc-NH-PEG4-CH2CH2COOH
    CAS: 756525-91-4

    Boc-NH-PEG4-CH2CH2COOH是一种基于PEG的PROTAClinker，用于合成PROTAC。Boc-NH-PEG4-CH2CH2COOH也是一种可降解的ADClinker，用于合成可降解的抗体偶联药物(ADC)的ADClinker。

  • GC60656 structure
    GC60656Boc-NH-PEG4-CH2CH2NH2
    CAS: 811442-84-9
    纯度: >97.00%

    Boc-NH-PEG4-CH2CH2NH2是一种可降解(cleavable)的5单元PEG类ADClinker，用于抗体偶联药物(ADC)的合成。

  • GC60658 structure
    GC60658Boc-Val-Dil-Dap-OH
    纯度: >99.50%

    Boc-Val-Dil-Dap-OH是一种ADC细胞毒素(ADCCytotoxin)。

  • GC60664 structure
    GC60664Br-PEG4-C2-Boc
    CAS: 564476-32-0

    Br-PEG4-C2-Boc是一种可降解(cleavable)的含4个单元PEG的ADClinker，可用于合成抗体偶联药物(ADC)。

  • GC60741 structure
    GC60741DBCO-CONH-S-S-NHS ester
    CAS: 1435934-53-4
    纯度: >95.00%

    DBCO-CONH-S-S-NHSester是一种可降解(cleavable)的ADClinker，可用于合成抗体偶联药物(ADC)。

  • GC60743 structure
    GC60743DBCO-PEG4-acetic-Val-Cit-PAB

    DBCO-PEG4-acetic-Val-Cit-PAB是一种可降解(cleavable)的含4个单元PEG的ADClinker，可用于合成抗体偶联药物(ADC)。

  • GC60848 structure
    GC60848Fmoc-3VVD-OH
    CAS: 863971-44-2

    Fmoc-3VVD-OH是一种可降解(non-cleavable)的ADC连接桥，用于抗体药物结合物(ADCs)的合成。

  • GC60849 structure
    GC60849Fmoc-Ala-Ala-Asn(Trt)-OH
    CAS: 1951424-92-2

    Fmoc-Ala-Ala-Asn(Trt)-OH是一种可降解(cleavable)的ADClinker，可用于合成抗体偶联药物(ADC)。

  • GC60850 structure
    GC60850Fmoc-Gly3-Val-Cit-PAB
    CAS: 2647914-09-6

    Fmoc-Gly3-Val-Cit-PAB是一种可降解(cleavable)的ADClinker，可用于合成抗体偶联药物(ADC)。

  • GC60851 structure
    GC60851Fmoc-NH-PEG1-CH2COOH
    CAS: 260367-12-2

    Fmoc-NH-PEG1-CH2COOH是一种可降解的ADClinker，用于抗体药物偶联物(ADC)合成。

  • GC60852 structure
    GC60852Fmoc-NH-PEG4-CH2CH2COOH
    CAS: 557756-85-1
    纯度: >98.00%

    Fmoc-NH-PEG4-CH2CH2COOH是一种可降解的ADClinker，用于抗体药物偶联物(ADC)合成。

  • GC60853 structure
    GC60853Fmoc-NH-PEG4-CH2COOH
    CAS: 437655-95-3

    Fmoc-NH-PEG4-CH2COOH是一种可降解的ADClinker，用于抗体药物偶联物(ADC)合成。

  • GC60870 structure
    GC60870Gemcitabine-O-Si(di-iso)-O-Mc
    纯度: >95.00%

    Gemcitabine-O-Si(di-iso)-O-Mc是抗体偶联药物的一部分，由嘧啶核苷类似物抗代谢药和抗肿瘤剂Gemcitabine和ADClinker连接而成。

  • GC61034 structure
    GC61034Mc-Val-Cit-PAB-Cl
    CAS: 1639351-92-0
    纯度: >95.00%

    Mc-Val-Cit-PAB-Cl是一种可降解的ADClinker，可用于连接MMAE和抗体，从而形成抗体-MC-vc-MMAE(如anti-CD22-MC-VC-PABC-MMAE，对BJAB和WSU具有细胞毒性，IC50分别为3.3nM和0.95nM)。

  • GC61047 structure
    GC61047Methotrexate disodium
    CAS: 7413-34-5
    纯度: >98.00%

    Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.

  • GC61101 structure
    GC61101N-(5-Hydroxypentyl)maleimide
    CAS: 180608-78-0
    纯度: >99.50%

    N-(5-Hydroxypentyl)maleimide是一种不可降解(non-cleavable)的ADClinker，可用于合成抗体偶联药物(ADC)，例如Gemcitabine-O-Si(di-iso)-O-Mc。

  • GC61112 structure
    GC61112N-Boc-diethanolamine
    CAS: 103898-11-9

    N-Boc-diethanolamine是一种可降解(cleavable)的ADClinker，用于抗体偶联药物(ADCs)的合成。

  • GC61113 structure
    GC61113N-Boc-PEG3-bromide
    CAS: 165963-71-3

    N-Boc-PEG3-bromide是一种可降解(cleavable)的ADClinker，用于抗体偶联药物(ADCs)的合成。

  • GC61128 structure
    GC61128NH2-PEG2-C2-Boc
    CAS: 756525-95-8
    纯度: >98.00%

    NH2-PEG2-C2-Boc是一种PROTAClinker，属于PEG类。NH2-PEG2-C2-Boc可用于合成PROTAC分子。NH2-PEG2-C2-Boc也是一种不可降解(non-cleavable)的含2个单元PEG的ADClinker，可用于合成抗体偶联药物(ADC)。

  • GC61131 structure
    GC61131NHS-PEG2-SS-PEG2-NHS
    纯度: >98.00%

    NHS-PEG2-SS-PEG2-NHS是一种可降解(cleavable)的含4个单元PEG的ADClinker，可用于合成抗体偶联药物(ADC)。

  • GC61207 structure
    GC61207Propargyl-PEG2-amine
    CAS: 944561-44-8
    纯度: >98.00%

    Propargyl-PEG2-amine是一种不可降解(non-cleavable)的ADClinker，用于抗体偶联药物(ADCs)的合成。Propargyl-PEG2-amine是一种PROTAClinker，属于PEG类。Propargyl-PEG2-NH2可用于合成一系列PROTAC分子。

  • GC61213 structure
    GC61213PROTAC BRD4 Degrader-5-CO-PEG3-N3
    纯度: >99.50%

    PROTACBRD4Degrader-5-CO-PEG3-N3(Compound2)一种用于PAC的PROTAC-linker偶联物，包含BRD4降解剂GNE-987和3个PEG的linker。