1. Cancer
  2. Cancer Targeted Therapy

Cancer Targeted Therapy (肿瘤靶向治疗)

Cancer targeted therapy is the foundation of precision medicine; it uses drugs or other substances to target specific genes and proteins that control cancer cells’ growth, division and spreading. Compared to traditional chemotherapy drugs, targeted-drugs can specifically act on cancer cells with high efficacy without damaging normal cells. Drugs used in cancer targeted therapy mainly includes small molecules and macromolecules (e.g., monoclonal antibodies), which can target cancer cells and constituents in the tumor microenvironment to activate the immune system. Anti-angiogenesis drugs, such as those targeting vascular endothelial growth factor (VEGF), epidermal growth factor receptor (EGFR), transforming growth factor (TGF)-α, TGF-β, Tumor necrosis factor (TNF)-α, and platelet-derived endothelial growth factor (PDGFR) inhibit the proliferation and metastasis of cancer cells. In recent years, the proportion of antibody drugs in cancer treatment has gradually become prominent. Antibody-drug conjugates (ADCs) are a new type of targeted drugs that are composed of monoclonal antibody, cytotoxic drug and linker. ADCs can deliver drugs to tumor cells and minimize the toxicity to normal tissues. Proteolysis-targeting chimera (PROTAC) is a useful technology for targeted protein degradation. PROTAC exploits the ubiquitin-proteasome system and forms a ternary complex with a hijacked E3 ubiquitin ligase and target protein, leading to polyubiquitination and degradation of the target protein.

Targeted therapy is a useful strategy in treatment of cancer either alone or in combination with standard chemotherapy. At present, targeted therapy has proved significant clinical success in the treatment of many types of cancer, including breast cancer, colorectal cancer, leukemia, ovarian cancer and lung cancer.

Cancer Targeted Therapy 相关产品 (35772):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-163239
    (R)-Thalidomide-piperazine-pyrrolidineethanol
    (R)-Thalidomide-piperazine-pyrrolidineethanol 是 E3 连接酶配体与连接子的缀合物 (E3 Ligase Ligand-Linker Conjugates),由 Thalidomide (HY-14658) 和对应 Linker 构成。(R)-Thalidomide-piperazine-pyrrolidineethanol 可作为 Cereblon 配体募集 CRBN 蛋白,并作为关键中间体进行完整 PROTACs 分子合成。
    (R)-Thalidomide-piperazine-pyrrolidineethanol
  • HY-147631
    KRAS G12C inhibitor 50 2760354-12-7
    KRAS G12C inhibitor 50 (Example 4) 是一种 KRAS G12C 抑制剂,IC50 值为 46.7 nM。
    KRAS G12C inhibitor 50
  • HY-168659
    E3 Ligase Ligand-linker Conjugate 130
    E3 Ligase Ligand-linker Conjugate 130 是一种 E3 泛素酶配体-连接子偶联物 (E3 ligase ligand-linker conjugate)。E3 Ligase Ligand-linker Conjugate 130 可用于合成 YJ1206 (HY-16855)。
    E3 Ligase Ligand-linker Conjugate 130
  • HY-140633
    Ald-C2-PEG4-azide 2030118-14-8
    Ald-C2-PEG4-azide 是一种 PROTAC linker,属于 PEG 类。可用于合成 PROTAC 分子。Ald-C2-PEG4-azide 是一种点击化学试剂。它含有 Azide 基团,可以和含有 Alkyne 基团的分子发生铜催化的叠氮-炔环加成反应(CuAAc)。它还可以和含有 DBCO 或 BCN 基团的分子发生环张力驱动的炔-叠氮环加成反应 (SPAAC)。
    Ald-C2-PEG4-azide
  • HY-RI03746
    mmu-miR-7006-3p inhibitor
    mmu-miR-7006-3p inhibitor 是一种全链经过甲氧基修饰的成熟miRNA的互补单链。miRNA inhibitor通过特异性结合成熟miRNA,阻止miRNA与其靶基因的互补配对,从而抑制miRNA的功能,可用于miRNA 功能缺失性(loss-of-function)研究。
    mmu-miR-7006-3p inhibitor
  • HY-116278
    HJC0149 1430330-65-6
    HJC0149 是一种有效的、具有口服活性的 transcription 3 (STAT3) 抑制剂。
    HJC0149
  • HY-140547
    NH-bis-PEG3 25743-12-8
    NH-bis-PEG3 是一种 PROTAC linker,属于 PEG 类。可用于合成 PROTAC 分子。
    NH-bis-PEG3
  • HY-RI00198
    hsa-miR-128-1-5p inhibitor
    hsa-miR-128-1-5p inhibitor 是一种全链经过甲氧基修饰的成熟miRNA的互补单链。miRNA inhibitor通过特异性结合成熟miRNA,阻止miRNA与其靶基因的互补配对,从而抑制miRNA的功能,可用于miRNA 功能缺失性(loss-of-function)研究。
    hsa-miR-128-1-5p inhibitor
  • HY-RI01396A
    hsa-miR-4770 antagomir
    hsa-miR-4770 antagomir 是一种经过特殊化学修饰的成熟miRNA的互补单链,全链进行甲氧基修饰,在5'端和3'端分别有2个和4个硫代骨架修饰,并在3'端连接有高亲和性胆固醇修饰。miRNA antagomir通过特异性结合成熟miRNA,阻止miRNA与其靶基因的互补配对,从而抑制miRNA的功能。相比于miRNA inhibitor,miRNA antagomir在动物实验中具有更高的稳定性和抑制效果,更易通过细胞膜、组织间隙而富集于靶细胞。
    hsa-miR-4770 antagomir
  • HY-19826
    Isofistularin-3
    Isofistularin-3 ((+)-11-epi-Fistularin 3) 是一种直接的 DNA 竞争性 DNMT1 抑制剂,IC50 为 13.5 μM。Isofistularin-3 作为 DNA 去甲基化剂,可诱导肿瘤细胞周期阻滞和 TRAIL 致敏。Isofistularin-3 可作用做抗体偶联活性分子 (ADC) 的毒素部分。
    Isofistularin-3
  • HY-151629
    MRV03-069 2797066-18-1
    MRV03-069 (化合物 3) 是一种选择性的大肠杆菌素活化肽酶 (ClbP) 抑制剂,能阻断 Colibactin (HY-145930) 对真核细胞的基因毒性作用。MRV03-069 可用于结肠直肠癌的研究。
    MRV03-069
  • HY-144831
    6BrCaQ-C10-TPP
    6BrCaQ-C10-TPP 是一种有效的线粒体热休克蛋白 TRAP1 抑制剂,在多种人类癌细胞中具有抗增殖活性 (IC50=0.008-0.30 μM)。6BrCaQ-C10-TPP 还可以诱导线粒体膜紊乱。
    6BrCaQ-C10-TPP
  • HY-157593
    E3 ligase Ligand-Linker Conjugate 35
    E3 ligase Ligand-Linker Conjugate 35 是 E3 连接酶配体与连接子的缀合物 (E3 Ligase Ligand-Linker Conjugates),由 (S,R,S)-AHPC (HY-125845) 和对应 Linker 构成。(S,R,S)-AHPC 是基于 VH032 的 von Hippel-Lindau (VHL) 配体,可募集 VHL 蛋白。E3 ligase Ligand-Linker Conjugate 35 可作为关键中间体进行完整 PROTACs 分子合成。
    E3 ligase Ligand-Linker Conjugate 35
  • HY-RI00485
    hsa-miR-24-2-5p inhibitor
    hsa-miR-24-2-5p inhibitor 是一种全链经过甲氧基修饰的成熟miRNA的互补单链。miRNA inhibitor通过特异性结合成熟miRNA,阻止miRNA与其靶基因的互补配对,从而抑制miRNA的功能,可用于miRNA 功能缺失性(loss-of-function)研究。
    hsa-miR-24-2-5p inhibitor
  • HY-144766
    ATX inhibitor 13 2485779-34-6
    ATX inhibitor 13 (compound 10c) 是一种口服有效的 ATX 抑制剂,其IC50 为 3.4 nM。ATX inhibitor 13 抑制 RAW264.7 细胞的增殖和迁移,诱导细胞凋亡和 G2 期阻滞。ATX inhibitor 13 抑制肿瘤细胞集落形成。
    ATX inhibitor 13
  • HY-RI04601
    rno-miR-9b-5p inhibitor
    rno-miR-9b-5p inhibitor 是一种全链经过甲氧基修饰的成熟miRNA的互补单链。miRNA inhibitor通过特异性结合成熟miRNA,阻止miRNA与其靶基因的互补配对,从而抑制miRNA的功能,可用于miRNA 功能缺失性(loss-of-function)研究。
    rno-miR-9b-5p inhibitor
  • HY-168515
    CDK9-IN-35
    CDK9-IN-35 (compound 10j) 是 CDK9/Cyclin T1 的抑制剂,其 IC50 值为 10.2 nM,对 HCT-116 细胞系的 IC50 值为 20 nM。
    CDK9-IN-35
  • HY-RI03995A
    mmu-miR-7229-3p antagomir
    mmu-miR-7229-3p antagomir 是一种经过特殊化学修饰的成熟miRNA的互补单链,全链进行甲氧基修饰,在5'端和3'端分别有2个和4个硫代骨架修饰,并在3'端连接有高亲和性胆固醇修饰。miRNA antagomir通过特异性结合成熟miRNA,阻止miRNA与其靶基因的互补配对,从而抑制miRNA的功能。相比于miRNA inhibitor,miRNA antagomir在动物实验中具有更高的稳定性和抑制效果,更易通过细胞膜、组织间隙而富集于靶细胞。
    mmu-miR-7229-3p antagomir
  • HY-140979
    Mal-amido-PEG8-TFP ester 1924596-31-5
    Mal-amido-PEG8-TFP ester 是一种 PROTAC linker,属于 PEG 类。可用于合成 PROTAC 分子。
    Mal-amido-PEG8-TFP ester
  • HY-157387
    c-Met-IN-22
    c-Met-IN-22(compound 51am) 是一种口服有效的 c-Met 抑制剂,IC50 值是 2.54 nM。c-Met-IN-22 具有抗增殖活性和抗肿瘤活性。c-Met-IN-22 可以诱导细胞凋亡(apoptosis)。
    c-Met-IN-22