2. Cancer
  3. Cancer Targeted Therapy

Cancer Targeted Therapy

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 Related Products (34003):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-RI02452A
    hsa-miR-8060 antagomir
    hsa-miR-8060 antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
    hsa-miR-8060 antagomir
  • HY-RI03252
    mmu-miR-5107-3p inhibitor
    mmu-miR-5107-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
    mmu-miR-5107-3p inhibitor
  • HY-150799
    CRBN ligand-1 3032314-67-0
    CRBN ligand-1 is a ligand for E3 ligase.
    CRBN ligand-1
  • HY-RI00486A
    hsa-miR-2467-3p antagomir
    hsa-miR-2467-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
    hsa-miR-2467-3p antagomir
  • HY-128355A
    (R)-IDO/TDO-IN-1 2033173-00-9 98.04%
    (R)-IDO/TDO-IN-1 (compound 25) is an indoleamine-2,3-dioxygenase (IDO) inhibitor, with good pharmacokinetic properties. (R)-IDO/TDO-IN-1 exhibits anti-tumor activity in MC38 xenograft model. (R)-IDO/TDO-IN-1 shows synergistic effect with anti-PD-1 monoclonal antibody (SHR-1210).
    (R)-IDO/TDO-IN-1
  • HY-119874
    Alkannin 23444-65-7
    Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent.
    Alkannin
  • HY-170763A
    (+)-Mcl-1 inhibitor 22 2332611-98-8
    (+)-Mcl-1 inhibitor 22 (Example 37) is a myeloid cell leukemia-1 (MCL-1) inhibitor which inhibits the antiapoptotoic activity of MCL-1 by inhibiting its interaction with proapototic proteins. (+)-Mcl-1 inhibitor 22 exhibits anti-proliferation activities against various cancer cell lines and can be utilized in cancer research.
    (+)-Mcl-1 inhibitor 22
  • HY-145023
    RET-IN-5 2725770-20-5
    RET-IN-5 is a potent RET (rearranged during transfection) inhibitor with an IC50s of 0.4 nM and 135.1 nM for RET and VEGFR2/KDR/Flk-1, respectively (WO2021213476A1, compound 18).
    RET-IN-5
  • HY-152208
    BPDA2 2907659-86-1
    BPDA2 is a highly selective and competitive active site SHP2 inhibitor with IC50s of 92.0 nM, 33.39 μM, 40.71 μM for SHP2, SHP1, SHP1B, respectively. DBDA2 downregulates mitogenic and cell survival signaling and RTK expression. BPDA2 suppresses SHP2 mediated signaling and breast cancer cell phenotypes.
    BPDA2
  • HY-10159S1
    Nilotinib-13C,d3 1261398-62-2
    Nilotinib-13C,d3 is a deuterated labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
    Nilotinib-<sup>13</sup>C,d<sub>3</sub>
  • HY-142965
    HDAC-IN-28 1621154-88-8
    HDAC-IN-28, a novel HDAC inhibitor, shows potent activities against tumor growth and metastasis
    HDAC-IN-28
  • HY-RI00360A
    hsa-miR-190a-3p antagomir
    hsa-miR-190a-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
    hsa-miR-190a-3p antagomir
  • HY-113921
    m-PEG4-propargyl 1101668-39-6
    m-PEG4-propargyl is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. m-PEG4-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    m-PEG4-propargyl
  • HY-168318
    Bestatin-amide-PEG3-CH2-acid
    Bestatin-amide-PEG3-CH2-acid is an E3 ligase ligand-linker conjugate. Bestatin-amide-PEG3-CH2-acid can be used to synthesize PROTAC RAR Degrader-1 (HY-111844).
    Bestatin-amide-PEG3-CH2-acid
  • HY-119357
    TN-16 33016-12-5 99.78%
    TN-16 is a potent inhibitor of microtubule polymerization with IC50 of 0.4-1.7 µM.
    TN-16
  • HY-140393
    N-(Tos-PEG4)-N-bis(PEG4-Boc) 2112737-74-1
    N-(Tos-PEG4)-N-bis(PEG4-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    N-(Tos-PEG4)-N-bis(PEG4-Boc)
  • HY-RI04256A
    rno-miR-1843b-3p antagomir
    rno-miR-1843b-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
    rno-miR-1843b-3p antagomir
  • HY-164632
    KRAS inhibitor-32 3056974-05-8
    KRAS inhibitor-32 (compound 139A) is a KRAS inhibitor. KRAS inhibitor-32 can be used in anti-cancer research.
    KRAS inhibitor-32
  • HY-111589
    EPZ-4777 1381761-52-9
    EPZ-4777 is a selective DOT1L inhibitor which inhibits H3K79 methylation in cancer cells, blocks the expression of leukemogenic genes, and selectively kills cells that contain the translocation. EPZ-4777 can be used for cancer research.
    EPZ-4777
  • HY-140425
    Boc-Aminooxy-PEG1-C2-NH2 1844894-82-1
    Boc-Aminooxy-PEG1-C2-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Boc-Aminooxy-PEG1-C2-NH2