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

Drug-Linker Conjugates for ADC

Antibody Drug Conjugates (ADC) are a rapidly expanding area in the pharmaceutical industry. They comprise of a desirable monoclonal antibody, an active cytotoxic drug and an appropriate linker. There are over 30 ADCs currently in pre-clinical or clinical development, and further improvements may be required to enhance the therapeutic potential of these ADCs. Monoclonal antibodies (mAbs) are of great use in many applications ranging from basic research to treatment of disease. The Drug-Linker Conjugates can expand the utility of mAbs and improve their potency and effectiveness; the antibodies are thus used as a means to target and delivery a toxic payload to the selected diseased tissue. The site-specific conjugations of Drug-Linker to an antibody may involve genetic engineering of the mAb to introduce discrete, available cysteines or non-natural amino acids with an orthogonally-reactive functional group handle such as an aldehyde, ketone, azido, or alkynyl tag. These site-specific approaches not only increase the homogeneity of ADCs but also enable novel bio-orthogonal chemistries that utilize reactive moieties other than thiol or amine. The cytotoxic drug, monomethyl auristatin E (MMAE), is conjugated to the three trastuzumab variants using a protease cleavable linker and shows in vivo therapeutic efficacy. The linker-MMAE conjugate is used in the U.S. FDA approved ADC, Brentuximab vedotin. There are also ADCs adopting linker-MMAE conjugate under clinical trials, such as Enfortumab vedotin and Glembatumumab vedotin.

Drug-Linker Conjugates for ADC 相关产品 (24):

Cat. No. Product Name Effect Purity
  • HY-15575
    VcMMAE 99.89%
    VcMMAE是抗体药物复合体的一部分 (drug-linker conjugate for ADC),具有抗癌活性,它由MMAE和Vc连接而成。
  • HY-19792
    Mertansine 98.74%
    Mertansine (DM1)是一种微管蛋白抑制剂,它在微管的末端结合并抑制微管的动态性。 Mertansine是一种抗体可缀合的美登木素生物碱,用于克服与美登素相关的全身毒性并增强肿瘤特异性递送。
  • HY-101070
    SMCC-DM1 99.54%
    SMCC-DM1是由连接桥SMCC和DM1连接而成的,用来制备抗体偶联药物。DM1 (mertansine),是含硫醇的美登木素生物碱,是一种有效的微管破坏剂。
  • HY-15578
    McMMAF 99.58%
    Mc-MMAF是由高效微管抑制剂Monomethyl auristatin F (MMAF) 与保护基团maleimidocaproyl偶联而成。MMAF(一甲基澳瑞他汀F)为抗微管蛋白化合物,能通过阻断微管聚合抑制细胞分裂,较MMAE毒性低,可用于抗体偶联药物(ADC)。
  • HY-111012
    DBCO-(PEG)3-VC-PAB-MMAE Chemical 98.07%
    DBCO-(PEG)3-VC-PAB-MMAE 由偶联于 DBCO-(PEG)3-vc-PAB 接头的 MMAE 制成。Monomethyl auristatin E (MMAE) 是一种有效的微管蛋白抑制剂,是抗体药物缀合物中的毒素有效载荷。
  • HY-112616
    NAMPT inhibitor-linker 2
    NAMPT inhibitor-linker 2 为 ADC 的一部分,由一种 NAMPT 的抑制剂作为有效载荷和一个连接物组成。ADC-4 由一个 NAMPT inhibitor-linker 2 和一个 anti-c-Kit 单克隆抗体组成,对表达 c-Kit 的细胞具有抑制作用,比如 GIST-T1 和 NCI-H526 细胞,IC50 值分别为 <7 pM 和 40 pM。
  • HY-111555
  • HY-114325
    SW-163D-AcLysValCit-PABC-DMAE是抗体药物复合体的一部分 (Drug-Linker Conjugates for ADC), 由天然的双嵌入剂SW-163D和连接桥AcLysValCitPABC-DMAE偶联构成。
  • HY-100566
  • HY-100567
    MAL-di-EG-Val-Cit-PAB-MMAE 99.57%
    MAL-di-EG-Val-Cit-PAB-MMAE是由高效微管抑制剂Monomethyl Auristatin E (MMAE)与多肽连接桥MAL-di-EG-Val-Cit-PAB偶联而成,是抗体偶联药物。
  • HY-100374
    Val-Cit-PAB-MMAE 99.83%
  • HY-100874
    N3-PEG3-vc-PAB-MMAE 99.18%
    N3-PEG3-vc-PAB-MMAE是 drug-linker conjugate for ADC的一部分, 由肽段N3-PEG3-vc-PAB和抗有丝分裂剂单甲基阿司他丁(MMAE) 连接而成。
  • HY-15741
    Mc-MMAE 是保护基团 (马来酰亚氨基己酰) 共轭连接到单甲基 auristatin E (MMAE)。Mc-MMAE 是有效的微管蛋白抑制剂,是抗体偶联药物 (ADC) 中的毒性物质。
  • HY-13631E
    Deruxtecan analog 99.43%
    Deruxtecan analog 是 DS-8201 的连接体,是一种毒素, 是连接桥与药物的偶联物,是抗体-药物偶联物 (ADC) 的一部分。详细信息请参考专利文献 WO2017002776A1 中的化合物 1。
  • HY-12460
    SPDB-DM4 是 ADC 的一部分,由 maytansinebased payload (DM4) 和 SPDB 连接而成,具有高效的抗肿瘤活性。
  • HY-19812
  • HY-19811
    Fmoc-Val-Cit-PAB-MMAE 98.89%
    Fmoc-Val-Cit-PAB-MMAE是由高效微管抑制剂Monomethyl auristatin E (MMAE)与多肽连接桥Fmoc-Val-Cit-PAB偶联而成,是抗体偶联药物。
  • HY-101141
    sulfo-SPDB-DM4 是 ADC 的一部分,由 maytansinebased payload (DM4) 与 sulfo-SPDB 连接而成。
  • HY-15740
    Mc-MMAE由高效微管抑制剂Monomethyl auristatin D(MMAD)与保护基团maleimidocaproyl偶联而成。
  • HY-15750
    Monomethyl auristatin D (MMAD)是微管蛋白抑制剂,是抗体偶联药物(ADC)中的毒素载荷。
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