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 (36579):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-18627A
    PFI-2 hydrochloride 1627607-87-7 99.48%
    PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0  nM and (S)-PFI-2 shows inhibiting activity with IC50  value of 1.0  μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.
    PFI-2 hydrochloride
  • HY-135899
    SIRT7 inhibitor 97491 1807758-81-1 98.81%
    SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
    SIRT7 inhibitor 97491
  • HY-126885
    DBCO-PEG5-NHS ester 2144395-59-3
    DBCO-PEG5-NHS ester is a PEG/Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs. DBCO-PEG5-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG5-NHS ester is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    DBCO-PEG5-NHS ester
  • HY-126682
    Mal-VC-PAB-DM1 1464051-44-2 99.41%
    Mal-VC-PAB-DM1 is a agent-linker conjugate for ADC with potent antitumor activity by using DM1 (a potent microtubule-disrupting agent), linked via the ADC linker Mal-VC-PAB .
    Mal-VC-PAB-DM1
  • HY-160444
    SJ3149 3026986-17-1 99.48%
    SJ3149 is a selective and potent molecular glue degrader of CK1α protein with broad antiproliferative activity. SJ3149 can be used in cancer research.
    SJ3149
  • HY-N0031
    Plantamajoside 104777-68-6 99.80%
    Plantamajoside is an orally active phenylpropanoid glycoside. Plantamajoside can be isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside inactivates NF-κB, PI3K/akt, induces Apoptosis, and improves Autophagy. Plantamajoside regulates MAPK, integrin-linked kinase/c-Src. Plantamajoside inhibits multiple cancers, improves lung and kidney damage. Plantamajoside has neuroprotective and anti-inflammatory effects.
    Plantamajoside
  • HY-136317
    MC-betaglucuronide-MMAE-1 1703778-92-0 99.23%
    MC-betaglucuronide-MMAE-1 is a agent-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.
    MC-betaglucuronide-MMAE-1
  • HY-145443
    Fludarabine-Cl 2734853-80-4 99.71%
    Fludarabine-Cl has an inhibitory effect on RNA adenosine deaminase 1 (ADAR1) with an IC50 of 0.87 μM and can be used to prevent and/or study cancer or tumor-related diseases.
    Fludarabine-Cl
  • HY-18669
    ML346 100872-83-1 98.25%
    ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 induces specific increases in genes and protein effectors of the heat shock response (HSR), including chaperones such as Hsp70, Hsp40, and Hsp27.
    ML346
  • HY-A0091A
    Pargyline 555-57-7 99.92%
    Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline has antihypertensive and anticancer activities. Pargyline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Pargyline
  • HY-A0276A
    Gentamicin 1403-66-3
    Gentamicin, an orally active aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. Gentamicin inhibits DNase I with an IC50 of 0.57 mM.
    Gentamicin
  • HY-32736
    Triptonide 38647-11-9 99.89%
    Triptonide (NSC 165677) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC50 of appropriately 0.3 nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects.
    Triptonide
  • HY-105129A
    Pimonidazole 70132-50-2 99.32%
    Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor. Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia .
    Pimonidazole
  • 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-U00459
    GSK2850163 2121989-91-9 98.25%
    GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
    GSK2850163
  • HY-10262
    BMS-536924 468740-43-4 99.83%
    BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity.
    BMS-536924
  • HY-100431
    IMR-1 310456-65-6 98.95%
    IMR-1 is a novel class of Notch inhibitor targeting the transcriptional activation with an IC50 of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth.
    IMR-1
  • 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-100355
    C18-Ceramide 2304-81-6 99.95%
    C18-Ceramide is a bioactive molecule with multiple functions in cells, can cross the blood-brain barrier, not a traditional agonist or inhibitor targeting a single site. It can act on multiple cellular targets, such as proteins related to endoplasmic reticulum stress (e.g., ATF-4, XBP-1, CHOP), proteins in the PI3K/AKT signaling pathway, and SNARE complex proteins. It exerts activities like inducing cell death, promoting autophagy, and regulating exocytosis through mechanisms such as activating endoplasmic reticulum stress, inhibiting the PI3K/AKT signaling pathway, and affecting lipid raft - related functions. It can be used in research on the mechanism of neuronal injury in the field of neuroscience and in the treatment research of cancers such as glioma in the field of oncology.
    C18-Ceramide