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.
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hCAIX-IN-3
0 ImagesCat. No.: HY-146983CAS No.: 2375461-31-5hCAII-IN-3 (compound 7e) is a potent and selective inhibitor of carbonic anhydrase (CA II/IX) with Kis of 124.2 and 30.5 nM, respectively. hCAII-IN-3 has the potential for the research of cancer diseases.
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HDAC-IN-45
0 ImagesCat. No.: HY-150577CAS No.: 2421122-61-2HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogen bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively.
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ILK-IN-4
0 ImagesCat. No.: HY-177912CAS No.: 1333146-87-4ILK-IN-4 (compound 49) is an integrin-linked kinase (ILK) inhibitor. ILK-IN-4 can be used for cancer research.
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hsa-miR-4797-5p inhibitor
0 ImagesCat. No.: HY-RI01438hsa-miR-4797-5p 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.
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hsa-miR-6751-3p antagomir
0 ImagesCat. No.: HY-RI02058Ahsa-miR-6751-3p 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.
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hDHODH-IN-11
0 ImagesCat. No.: HY-151560CAS No.: 2396653-34-0hDHODH-IN-11 is a potent human dihydroorotate dehydrogenase (hDHODH) inhibitor with an IC50 value of 7.2 nM. hDHODH-IN-11 has low cytotoxicity. hDHODH-IN-11 can be used in research of acute myeloid leukemia (AML).
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EGFR/HER2/CDK9-IN-1
0 ImagesCat. No.: HY-147796CAS No.: 879730-44-6
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NSCLC-IN-1
0 ImagesCat. No.: HY-161388NSCLC-IN-1 (Compound A10-2) induces mitophagy and ferroptosis through targeting transmembrane BAX inhibitor motif containing 6 (TMBIM6). NSCLC-IN-1 induces mitochondrial Ca2+ imbalance, leading to mitochondrial damage. NSCLC-IN-1 reduces intracellular glutathione (GSH), increases the accumulation of lipid peroxides (LPO) and malondialdehyde (MDA) content. NSCLC-IN-1 is a potent anti-NSCLC agent.
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Thalidomide-NH-amido-C4-Br
0 ImagesCat. No.: HY-170307CAS No.: 3027457-50-4Thalidomide-NH-amido-C4-Br is a conjugate of the E3 ligase ligand and the linker, that can be used for synthesis of PROTAC degrader BSJ-02-162 (HY-144995).
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MI-773 TFA
0 ImagesMI-773 TFA is an orally active, selective MDM2-p53 interaction inhibitor with a Ki of 0.88 nM for MDM2. MI-773 TFA blocks the MDM2-TP53 interaction. MI-773 TFA potently activates p53. MI-773 TFA induces Apoptosis. MI-773 TFA causes tumor regression in xenograft models of adenoid cystic carcinoma. MI-773 TFA exhibits anticancer effects in neuroblastoma. MI-773 TFA can be used for the research of adenoid cystic carcinoma.
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hsa-miR-4287 inhibitor
0 ImagesCat. No.: HY-RI00966hsa-miR-4287 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.
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hsa-miR-5197-5p antagomir
0 ImagesCat. No.: HY-RI01586Ahsa-miR-5197-5p 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.
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Boc-amino-PEG3-SSPy
0 ImagesCat. No.: HY-136041CAS No.: 2740153-37-9Boc-amino-PEG3-SSPy is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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hsa-miR-769-3p inhibitor
0 ImagesCat. No.: HY-RI02415hsa-miR-769-3p 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.
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mmu-miR-342-5p inhibitor
0 ImagesCat. No.: HY-RI03037mmu-miR-342-5p 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.
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mmu-miR-6967-5p inhibitor
0 ImagesCat. No.: HY-RI03662mmu-miR-6967-5p 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.
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rno-miR-200b-3p inhibitor
0 ImagesCat. No.: HY-RI04283rno-miR-200b-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.
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VEGFR-2-IN-83
0 ImagesCat. No.: HY-182032VEGFR-2-IN-83 is a VEGFR-2 kinase inhibitor with an IC50 of 0.037 μM. VEGFR-2-IN-83 induces G0/G1 cell cycle arrest and apoptosis in breast cancer cells, and increases the production of reactive oxygen species (ROS). VEGFR-2-IN-83 is applicable to relevant research on breast cancer.
