1. Signaling Pathways
  2. Antibody-drug Conjugate/ADC Related
  3. ADC Linker

ADC Linker

Antibody-drug conjugates (ADCs) consist of a desirable monoclonal antibody, an active cytotoxic drug and an appropriate linker. An appropriate linker between the antibody and the cytotoxic drug provides a specific bridge, and thus helps the antibody to selectively deliver the cytotoxic drug to tumor cells and accurately releases the cytotoxic drug at tumor sites. In addition to conjugation, the linkers maintain ADCs’ stability during the preparation and storage stages of the ADCs and during the systemic circulation period.

The ADCs currently undergoing clinical evaluation contain linkers are mostly classified into two categories: cleavable and noncleavable. Cleavable linkers rely on processes inside the cell to liberate the toxin, such as reduction in the cytoplasm, exposure to acidic conditions in the lysosome, or cleavage by specific proteases within the cell. Noncleavable linkers require proteolytic degradation of the antibody portion of the ADC for release of the cytotoxic molecule, which will retain the linker and the amino acid by which it was attached to the antibody.

The selection of linker is target dependent, based on the knowledge of the internalization and degradation of the antibody-target antigen complex, and a preclinical in vitro and in vivo activity comparison of conjugates. Moreover, the choice of a linker is also influenced by which cytotoxin is used, as each molecule has different chemical constraints, and frequently the drug structure lends itself to a specific linker.

ADC Linker 相关产品 (39):

Cat. No. Product Name Effect Purity
  • HY-78738
    MC-Val-Cit-PAB 99.69%
    MC-Val-Cit-PAB是可被组织蛋白酶切割的ADC连接桥,用于制备抗体-药物偶联物。 美国FDA批准的药物,如brentuximab vedotin使用了该连接桥。
  • HY-12362
    Val-cit-PAB-OH 99.64%
    Val-cit-PAB-OH是一种多肽前体药物连接子。
  • HY-41189
    Fmoc-Val-Cit-PAB-PNP
    Fmoc-Val-Cit-PAB-PNP是一种多肽前体药物连接子,是抗体偶联药物 (ADC) 的常用连接桥。
  • HY-20336
    Mc-Val-Cit-PABC-PNP 98.68%
    Mc-Val-Cit-PABC-PNP是用于合成抗体-药物偶联物 (ADCs) 的,可切割的组织蛋白酶连接桥 (ADC linker)。
  • HY-43869
    Vipivotide tetraxetan Linker
    Vipivotide tetraxetan Linker 是一种有效的肽类接头,可用于合成 Vipivotide tetraxetan (PSMA-617)。 Vipivotide tetraxetan (PSMA-617) 是用于合成 177Lu-PSMA-617 的配体,177Lu-PSMA-617 是用于治疗前列腺癌的一种放射性分子。
  • HY-101159
    Mal-amido-PEG8-acid
    Mal-amido-PEG8-acid (example 143) 是一个ADC 连接桥,信息来自专利US2018339985。
  • HY-128946
    CL2A-SN-38
    CL2A-SN-38,SN-38 衍生物,肽连接体。CL2A-SN-38 与抗 Trop-2 人源化抗体缀合,形成抗体药物偶联物 (ADC),针对人类实体瘤表现出特异性的抗肿瘤作用。
  • HY-114430
    Fmoc-Phe-Lys(Boc)-PAB-PNP 98.67%
    Fmoc-Phe-Lys(Boc)-PAB-PNP 是抗体偶联药物 (ADC) 的常用连接桥。
  • HY-78961
    6-Maleimidohexanoic acid N-hydroxysuccinimide ester 99.96%
    6-Maleimidohexanoic acid N-hydroxysuccinimide ester(ECMS)是抗体偶联药物(ADC)中常用保护基团。
  • HY-19318
    Fmoc-Val-Cit-PAB 98.13%
    Fmoc-Val-Cit-PAB是抗体偶联药物(ADC)的常用连接桥。
  • HY-21210
    6-Quinoxalinecarboxylic acid, 2,3-bis(bromomethyl)-
    6-Quinoxalinecarboxylic acid, 2,3-bis(bromomethyl)- 是抗体偶联药物 (ADC) 的连接桥。
  • HY-128957
    Modified MC-VC-PABC
    Modified MC-VC-PABC 是用于合成抗体药物复合体的,不可切割的 ADC 连接桥 (ADC linker) 。
  • HY-128927
    Mc-Leu-Gly-Arg
    Mc-Leu-Gly-Arg 是一种醚类 linker,可用于抗体-药物偶联物 (ADC) 研究。
  • HY-128944
    MAC glucuronide linker
    MAC glucuronide linker 是一种用于抗体药物复合物 (ADCs) 的连接桥,可用于制备 MAC glucuronide SN-38 药物连接桥。
  • HY-128954
    Sulfo-SPDB linker
    Sulfo-SPDB linker 用于抗体-药物缀合物 (ADC),可切割性二硫键 linker。
  • HY-W000438
    N-Boc-O-tosyl hydroxylamine
    N-Boc-O-tosyl hydroxylamine 可用作抗体偶联药物 (ADC) 的连接桥。
  • HY-128929
    Fmoc-PEA
    Fmoc-PEA (Example 1-2) 可用作抗体偶联药物 (ADC) 的连接桥。
  • HY-128947
    CL2 Linker
    CL2 Linker 是 ADC 分子的一个连接桥。CL2-SN-38 和 CL2A-SN-38 拥有几乎等效的药物替代 (~6)、细胞结合 (Kd ~1.2 nM)、细胞毒性 (IC50 ~2.2 nM) 以及体外血清稳定性 (t1/2 ~20 小时)。
  • HY-112099
    Mc-Val-Cit-PAB-Cl
    Mc-Val-Cit-PAB-Cl 是一种 ADC linker,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 3.3 nM 和 0.95 nM)。
  • HY-128960
    SPDB-DM4 linker
    SPDB-DM4 linker 用于抗体-药物缀合物 (ADC) 的可切割性谷胱甘肽接头。
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