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 (35606):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-132868
    SLK/STK10-IN-1 264210-49-3 99.78%
    SLK/STK10-IN-1 is a potent and selective inhibitor of SLK and STK10 with antitumor activity.
    SLK/STK10-IN-1
  • HY-P1416A
    Foxy-5 TFA 99.02%
    Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
    Foxy-5 TFA
  • HY-10617
    Rucaparib phosphate 459868-92-9 99.76%
    Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research.
    Rucaparib phosphate
  • HY-119339
    SX-682 1648843-04-2 99.67%
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
    SX-682
  • HY-13866
    Ro 31-8220 mesylate 138489-18-6 99.57%
    Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
    Ro 31-8220 mesylate
  • HY-100848
    TX1-85-1 1603845-32-4 98.28%
    TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
    TX1-85-1
  • HY-15245
    GSK2636771 1372540-25-4 99.59%
    GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
    GSK2636771
  • HY-10518
    BMS-345541 hydrochloride 547757-23-3 99.90%
    BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
    BMS-345541 hydrochloride
  • HY-70044
    GSK-1070916 942918-07-2 99.55%
    GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
    GSK-1070916
  • HY-100548
    GSK621 1346607-05-3 98.03%
    GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
    GSK621
  • HY-128918
    SIS17 2374313-54-7 99.65%
    SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM. SIS17 inhibits the demyristoylation of serine hydroxymethyltransferase 2, a substrate of HDAC 11, but does not inhibit other HDACs.
    SIS17
  • HY-17567B
    Heparin Lithium salt 9045-22-1
    Heparin Lithium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII). Heparin Lithium salt significantly inhibits exosome-cell interactions.
    Heparin Lithium salt
  • HY-147041
    Selvigaltin 1978336-95-6 98.87%
    Selvigaltin (GB1211) is an orally active galectin-3 small molecule inhibitor with an IC50 value of 12 nM in rabbits, showing anti-tumor activity. Selvigaltin decreases galectin-3 levels in the liver and reduces biomarkers of liver function (AST, ALT, bilirubin), inflammation (cells foci) and fibrosis (PSR, SHG), as well as decreasing the mRNA and protein expression of several key inflammation and fibrosis biomarkers (IL6, TGFβ3, SNAI2, collagen). Selvigaltin restores T-cell activity and induces less tumors and metastasis.
    Selvigaltin
  • HY-15542B
    FRAX486 1232030-35-1 98.01%
    FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
    FRAX486
  • HY-15967
    PS48 1180676-32-7 99.71%
    PS48 is an activator of PDK1 with an AC50 of 8 μM.
    PS48
  • HY-11005
    BX-912 702674-56-4 99.13%
    BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
    BX-912
  • HY-139612
    Opnurasib 2653994-08-0 98.71%
    Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity.
    Opnurasib
  • HY-13643
    Daminozide 1596-84-5 99.79%
    Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC50s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested.
    Daminozide
  • HY-148026
    Sonrotoclax 2383086-06-2 99.61%
    Sonrotoclax is a potent, orally active Bcl2 inhibitor. Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines.
    Sonrotoclax
  • HY-15513
    TC-DAPK 6 315694-89-4
    TC-DAPK 6 is a potent, ATP-competitive, and highly selective DAPK inhibitor (IC50=69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP).
    TC-DAPK 6