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-B0656S1
    Rabeprazole-13C,d3 1261392-48-6
    Rabeprazole-13C,d3 is a deuterated labeled Rabeprazole. Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux.
    Rabeprazole-<sup>13</sup>C,d<sub>3</sub>
  • HY-16985R
    Darolutamide (Standard) 1297538-32-9
    Darolutamide (Standard) is the analytical standard of Darolutamide. This product is intended for research and analytical applications. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
    Darolutamide (Standard)
  • HY-12933
    BIIB-028 911398-13-5
    BIIB-028 is an orally active inhibitor for heat shock protein 90 (Hsp90). BIIB-028 targets the ATP-binding site of Hsp90, disrupts the function of Hsp90, leads to the degradation of client proteins, that are crucial for cancer cell survival and proliferation.
    BIIB-028
  • HY-47733
    CDK1/2/4-IN-2 677701-62-1
    WAY-643018 (Compound 2), an indazolecarboxamide derivative, is a CDK1, CDK2, and CDK4 inhibitor. CDK1/2/4-IN-2 has the potential for cancer research.
    CDK1/2/4-IN-2
  • HY-122626
    BRPF1B/TRIM24-IN-1 1242907-48-7
    BRPF1B/TRIM24-IN-1 (compound 34) is a potent TRIM24/BRPF1/BRPF2 inhibitor, with IC50 values of 0.43, 0.34, 1.75 μM, respectively. BRPF1B/TRIM24-IN-1 binds the TRIM24 bromodomain with a KD of 222 nM and has a KD for the BRPF1 bromodomain of 137 nM and for BRD1 of 1130 nM.
    BRPF1B/TRIM24-IN-1
  • HY-W190924
    Mal-amido-PEG8-val-gly 2353409-54-6
    Mal-amido-PEG8-Val-Gly is an ADC linker containing a maleimide group.
    Mal-amido-PEG8-val-gly
  • HY-124953R
    7,3',4'-Trihydroxyisoflavone (Standard) 485-63-2
    7,3',4'-Trihydroxyisoflavone (Standard) is the analytical standard of 7,3',4'-Trihydroxyisoflavone. This product is intended for research and analytical applications. 7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities.
    7,3',4'-Trihydroxyisoflavone (Standard)
  • HY-112502A
    MethADP disodium 104835-70-3
    MethADP disodium is a specific CD73 inhibitor.
    MethADP disodium
  • HY-172295
    Tetrafluoro-thalidomide 179033-21-7
    Tetrafluoro-thalidomide is a fluorinated Thalidomide analogue. Tetrafluoro-thalidomide is an activator of E3 ligase, which ubiquitinylates proteins for later proteolysis. The structure may be further derivatized via substitution at its fluorines.
    Tetrafluoro-thalidomide
  • HY-119975
    Carazostatin 126168-32-9
    Carazostatin (DC118), an antioxidant, can be isolated from Streptomycs chromofuscus. Carazostatin (DC118) exhibits strong inhibitory activity against free radical-induced lipid peroxidation and shows stronger antioxidant activity in liposomal membranes than α-tocopherol (VE).
    Carazostatin
  • HY-137139
    10'-Desmethoxystreptonigrin 136803-89-9
    10'-Desmethoxystreptonigrin is an inhibitor for Ras Farnesyltransferase with an IC50 of 21 μM. 10'-Desmethoxystreptonigrin is a broad-spectrum antibiotic with antibacterial activity. 10'-Desmethoxystreptonigrin exhibits antitumor activity against P388 leukemia, without significant cytotoxicity (LD50 is 8.8 mg/kg).
    10'-Desmethoxystreptonigrin
  • HY-160174A
    BCR-ABL kinase-IN-3 (dihydrocholide)
    BCR-ABL kinase-IN-3 (dihydrocholide) (example 1) is a potent inhibitor of BCR-ABL that plays an important role in acute myeloid leukemia (AML) research.
    BCR-ABL kinase-IN-3 (dihydrocholide)
  • HY-12177R
    Aliskiren hemifumarate (Standard) 173334-58-2
    Aliskiren (hemifumarate) (Standard) is the analytical standard of Aliskiren (hemifumarate). This product is intended for research and analytical applications. Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
    Aliskiren hemifumarate (Standard)
  • HY-137632
    Sp-8-Cl-cAMPS 142754-28-7
    Sp-8-Cl-cAMPS is an analog of cAMP (HY-B1511) and a derivative of Sp-8-Cl-cAMP. Sp-8-Cl-cAMPS inhibits the growth of human leukemia cell HL-60 and colon cancer cell LS-174T, with IC50 of 8-100 μM. Sp-8-Cl-cAMPS activates the protein kinases cAKI and cAKII, with Ka of 0.25 and 3.2 μM.
    Sp-8-Cl-cAMPS
  • 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-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