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 (35605):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-13734
    PX-12 141400-58-0 99.87%
    PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively.
    PX-12
  • HY-137331
    FAPI-46 2374782-04-2 98.57%
    FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted tracer. Use radioactivity FAPI-46 labeled with 68Ga or 177Lu can be used for tumor imaging in a variety of cancers and has higher tumor uptake rates and longer tumor accumulation.
    FAPI-46
  • HY-W021377
    Exatecan Intermediate 2 182182-31-6 99.99%
    Exatecan Intermediate 2 (Compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers.
    Exatecan Intermediate 2
  • HY-160701
    Cirtociclib 2888704-84-3 99.02%
    Cirtociclib (BLU-222) is an orally active and highly selective CDK2 inhibitor. Cirtociclib disrupts Rb signaling and causes G1 arrest and apoptosis in CCNE1-amplified endometrial cancer cells.
    Cirtociclib
  • HY-109103
    Tegatrabetan 1227637-23-1 99.84%
    Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).
    Tegatrabetan
  • HY-N0036
    Costunolide 553-21-9 99.69%
    Costunolide ((+)-Costunolide) is a naturally occurring sesquiterpene lactone, with antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Costunolide can induce cell cycle arrest and apoptosis on breast cancer cells.
    Costunolide
  • HY-15247
    Vistusertib 1009298-59-2 99.32%
    Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
    Vistusertib
  • HY-13241
    Ralimetinib dimesylate 862507-23-1 99.94%
    Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
    Ralimetinib dimesylate
  • HY-A0014
    Ramelteon 196597-26-9 99.87%
    Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
    Ramelteon
  • HY-N0077
    Ginkgolic Acid 22910-60-7 99.91%
    Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
    Ginkgolic Acid
  • HY-16704
    ESI-09 263707-16-0 99.65%
    ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.
    ESI-09
  • HY-130208
    Thiodigalactoside 51555-87-4 99.97%
    Thiodigalactoside (TDG) is an orally active and potent galectin (GAL) inhibitor with Kd values of 24 μM, 49 μM for GAL1 and GAL3, respectively. Thiodigalactoside, a non-metabolizable disaccharide, has anti-inflammatory and anti-cancer activity. Thiodigalactoside dramatically reduces body weight gain in diet-induced obese rats.
    Thiodigalactoside
  • HY-15594A
    Phen-DC3 Trifluoromethanesulfonate 929895-45-4 98.99%
    Phen-DC3 Trifluoromethanesulfonate is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65±6 and 50±10 nM, respectively.
    Phen-DC3 Trifluoromethanesulfonate
  • HY-Y0248A
    Farnesol 4602-84-0 99.88%
    Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
    Farnesol
  • HY-13773
    Motolimod 926927-61-9 98.12%
    Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM.
    Motolimod
  • HY-110404
    Capzimin 2084868-04-0 99.19%
    Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
    Capzimin
  • HY-14885
    Eliglustat 491833-29-5 99.95%
    Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
    Eliglustat
  • HY-B0492
    Paroxetine hydrochloride 78246-49-8 99.96%
    Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder.
    Paroxetine hydrochloride
  • HY-17406
    Tolcapone 134308-13-7 99.86%
    Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma.
    Tolcapone
  • HY-137435
    Cirtuvivint 2143917-62-6 98.28%
    Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor. Cirtuvivint can be used for solid tumors research.
    Cirtuvivint