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 (35020):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-13962
    SGI-1027 1020149-73-8 99.77%
    SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
    SGI-1027
  • HY-102080
    SAFit2 1643125-33-0 98.59%
    SAFit2 is a highly potent, highly selective FK506-binding protein 51 (FKBP51) inhibitor with a Ki of 6 nM and also enhances AKT2-AS160 binding.
    SAFit2
  • HY-B0034
    Donepezil Hydrochloride 120011-70-3 99.92%
    Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.
    Donepezil Hydrochloride
  • HY-P99033
    Mosunetuzumab 1905409-39-3 99.05%
    Mosunetuzumab (BTCT-4465A) is a full-length, fully humanized immunoglobulin G1 (IgG1) T-cell-dependent bispecific (TDB) antibody targeting CD20 (B cells) and CD3 (T cells). Mosunetuzumab redirects T cells to engage and eliminate malignant B cells and can be used for the research of relapsed or refractory (R/R) B-cell non-Hodgkin lymphomas (B-NHLs).
    Mosunetuzumab
  • HY-N0018
    Daidzin 552-66-9 99.77%
    Daidzin is an isoflavone with antioxidant, anticancer, and antiatherosclerotic activities. Daidzin is a potent and selective inhibitor of mitochondrial ALDH-2. Daidzin reduces ethanol consumption.
    Daidzin
  • HY-10249A
    AKT Kinase Inhibitor 842148-40-7 99.92%
    AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity.
    AKT Kinase Inhibitor
  • HY-112301
    Pralsetinib 2097132-94-8 99.98%
    Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively.
    Pralsetinib
  • HY-16168A
    Degarelix 214766-78-6 99.94%
    Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing hormone (GnRH) receptor (IC50 = 3 nM). Degarelix acetate Degarelix acetate (FE 200486) is used for the research of prostate cancer.
    Degarelix
  • HY-18361
    TMP195 1314891-22-9 99.82%
    TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with Kis of 59, 60, 26, 15 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
    TMP195
  • HY-18682
    Centrinone 1798871-30-3 98.28%
    Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM.
    Centrinone
  • HY-128359
    ACBI1 2375564-55-7 99.92%
    ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis.
    ACBI1
  • HY-16582A
    Sonidegib 956697-53-3 99.94%
    Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.
    Sonidegib
  • HY-10578
    PD 169316 152121-53-4 98.29%
    PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC50 of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.
    PD 169316
  • HY-Q45780
    ZINC00640089 667880-11-7 99.95%
    ZINC00640089 is a specific Lipocalin-2 (LCN2) inhibitor. ZINC00640089 inhibits cell proliferation, cell viability and reduces AKT phosphorylation levels in SUM149 cells. ZINC00640089 has good potential for research in inflammatory breast cancer (IBC).
    ZINC00640089
  • HY-101092
    QS-21 141256-04-4 99.67%
    QS-21, an immunostimulatory saponin, could be used as a potent vaccine adjuvant. QS-21 stimulates Th2 humoral and Th1 cell-mediated immune responses through action on antigen presenting cells (APCs) and T cells. QS-21 can activate the NLRP3 inflammasome with subsequent release of caspase-1 dependent cytokines, IL-1β and IL-18.
    QS-21
  • HY-100508
    ITSA-1 200626-61-5 99.73%
    ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation.
    ITSA-1
  • HY-12987
    Pimozide 2062-78-4 99.91%
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
    Pimozide
  • HY-118630
    Vacuolin-1 351986-85-1 98.93%
    Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation. Vacuolin-1 can induce vacuole formation and increase the percentage of enucleated cells.
    Vacuolin-1
  • HY-N0045
    Ginsenoside Rg1 22427-39-0 99.91%
    Ginsenoside Rg1 is one of the major active components of Panax ginseng. Ginsenoside Rg1 ameliorates the impaired cognitive function, displays promising effects by reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces NF-κB nuclear translocation.
    Ginsenoside Rg1
  • HY-10981A
    Lenvatinib mesylate 857890-39-2 99.86%
    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
    Lenvatinib mesylate