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 (36474):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-159937
    PKMYT1-IN-7 2986404-30-0
    PKMYT1-IN-7 (compound 7) is an orally active PKMYT1 inhibitor with IC50 values of 1.6 nM and 0.06 μM against of PKMYT1 and pCDK1, respectively. PKMYT1-IN-7 suppresses the phosphorylation of CDK1 at T14 and Y15. PKMYT1-IN-7 shows anticancer activity both < and <.
    PKMYT1-IN-7
  • HY-113759
    Saquayamycin A 99260-65-8
    Saquayamycin A has antimicrobial effect, but it has weaker effect against Gram-negative bacteria. Saquayamycin A has inhibitory effect on leukemia P388 cells and Adriamycin-resistant P388 cells.
    Saquayamycin A
  • HY-18690R
    Enasidenib (Standard) 1446502-11-9
    Enasidenib (Standard) is the analytical standard of Enasidenib. This product is intended for research and analytical applications. Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively.
    Enasidenib (Standard)
  • HY-157503
    Photosensitizer-3 1928742-39-5
    Photosensitizer-3 is a photosensitizer that exhibits powerful selective killing effects on transfected HEK cells and affibody-targeted A431 cancer cells when exposed to near-infrared light excitation.
    Photosensitizer-3
  • HY-168649
    JH-LPH-107 3053068-92-8
    JH-LPH-107 is a LpxH inhibitor. JH-LPH-107 exhibits a low rate of spontaneous resistance and a high safety window in vitro..
    JH-LPH-107
  • HY-N0102R
    Isoliquiritigenin (Standard) 961-29-5
    Isoliquiritigenin (Standard) is the analytical standard of Isoliquiritigenin. This product is intended for research and analytical applications. Isoliquiritigenin is an anti-tumor flavonoid from the root of Glycyrrhiza uralensis Fisch., which inhibits aldose reductase with an IC50 of 320 nM. Isoliquiritigenin is a potent inhibitor of influenza virus replication with an EC50 of 24.7 μM.
    Isoliquiritigenin (Standard)
  • HY-164588
    NH2-PEG4-NODA-GA 2306108-46-1
    NH2-PEG4-NODA-GA is a NODA-type metal chelator that can bind to radionuclides to prepare radionuclide drug conjugates (RDCs). RDCs have the ability to specifically target biomolecules and can be used in medical imaging or therapy.
    NH2-PEG4-NODA-GA
  • HY-13521R
    SB-505124 (Standard) 694433-59-5
    SB-505124 (Standard) is the analytical standard of SB-505124. This product is intended for research and analytical applications. SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
    SB-505124 (Standard)
  • HY-101849R
    Fasentin (Standard) 392721-37-8
    Fasentin (Standard) is the analytical standard of Fasentin. This product is intended for research and analytical applications. Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.
    Fasentin (Standard)
  • HY-10255AR
    Sunitinib (Standard) 557795-19-4
    Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
    Sunitinib (Standard)
  • HY-133362
    Fmoc-NH-PEG16-CH2CH2COOH
    Fmoc-NH-PEG16-CH2CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Fmoc-NH-PEG16-CH2CH2COOH
  • HY-164393
    ON044580 1035199-04-2
    ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling.
    ON044580
  • HY-122585
    proMMP-9 inhibitor-3c 2138321-18-1
    proMMP-9 inhibitor-3c (compound 3c) is a potent proMMP-9 inhibitor. proMMP-9 inhibitor-3c is specific for binding to the proMMP-9 hemopexin-like domain (Kd=320 nM). proMMP-9 inhibitor-3c disruption of MMP-9 homodimerization prevents association of proMMP-9 with both α4β1 integrin and CD44 and results in the dissociation of EGFR. This disruption results in decreased phosphorylation of Src and its downstream target proteins focal adhesion kinase (FAK) and paxillin (PAX).
    proMMP-9 inhibitor-3c
  • HY-168145
    MAGL-IN-19 2411570-42-6
    MAGL-IN-19 (compund 7o) is a highly potent and selective MAGL inhibitor.
    MAGL-IN-19
  • HY-168667
    E3 ligase Ligand 40
    E3 ligase Ligand 40 is a conjugate of E3 ligase ligand and linker that serve as a key intermediate for the synthesis of complete PROTAC molecule CPD-39 (HY-168664).
    E3 ligase Ligand 40
  • HY-101561R
    Avapritinib (Standard) 1703793-34-3
    Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.
    Avapritinib (Standard)
  • HY-169735
    Aurora A inhibitor 4 371224-09-8
    Aurora A inhibitor 4 (compound C9) is a potent inhibitor of Aurora A, with the GI50 of 4.26 and 7.08 μM in DU 145 cells and HT-29 cells, respectively.
    Aurora A inhibitor 4
  • HY-161472
    Aldose reductase-IN-7
    Aldose reductase-IN-7 (Compound 6k) targets Aldose reductase. Aldose reductase-IN-7 exhibits potent enzyme inhibitory activity (Ki = 0.186 ± 0.020 μM), showing superiority to Epalrestat (HY-66009), which is currently in clinical use. Aldose reductase-IN-7 is less cytotoxic and possesses potent anticancer activity.
    Aldose reductase-IN-7
  • HY-13646AR
    Encequidar mesylate (Standard) 849675-87-2
    Encequidar (mesylate) (Standard) is the analytical standard of Encequidar (mesylate). This product is intended for research and analytical applications. Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
    Encequidar mesylate (Standard)
  • HY-20560
    (Ac)Phe-Lys(Alloc)-PABC-PNP 2070009-39-9
    (Ac)Phe-Lys(Alloc)-PABC-PNP is an useful cleavable chemical linker in antibody drug conjugates.
    (Ac)Phe-Lys(Alloc)-PABC-PNP