1. Cancer
  2. 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 (34635):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-15409S1
    Empagliflozin-13C6
    Empagliflozin-13C6 (BI 10773-13C6) is 13C labeled Empagliflozin. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2.
    Empagliflozin-<sup>13</sup>C<sub>6</sub>
  • HY-10212R
    BIIB021 (Standard) 848695-25-0
    BIIB021 (Standard) is the analytical standard of BIIB021. This product is intended for research and analytical applications. BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a Ki and an EC50 of 1.7 nM and 38 nM, respectively[1].
    BIIB021 (Standard)
  • HY-133360
    Cbz-NH-PEG36-C2-acid
    Cbz-NH-PEG36-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Cbz-NH-PEG36-C2-acid
  • HY-138215
    ADTL-EI1712 2414916-45-1
    ADTL-EI1712 is a potent, orally active, and selective dual-target inhibitor of ERK1 and ERK5, inhibition rates of ERK1/5 at 1 μM are 93.54% and 89.35%, respectively. ADTL-EI1712 can induce regulated cell death, a form of cell death that relies on the activation of genetically encoded machinery, to overcome compensatory mechanism in specific cancer cells in vitro and in vivo.
    ADTL-EI1712
  • HY-A0032
    Valganciclovir 175865-60-8
    Valganciclovir, the L-valyl ester of ganciclovir, is actually a prodrug for ganciclovir.
    Valganciclovir
  • HY-118403
    CK2-IN-12 300675-28-9
    CK2-IN-12 (Compound 39) is an inhibitor for protein kinase CK2 with an IC50 of 0.8 μM.
    CK2-IN-12
  • HY-163725
    DHFR-IN-18
    DHFR-IN-18 (compound 19D) is a DHFR inhibitor. DHFR-IN-18 can be used in anti-leukemia research.
    DHFR-IN-18
  • HY-162580
    SphK2-IN-3
    SphK2-IN-3 (compound 12q) is a selective active sphingosine kinase-2 inhibitor. SphK2-IN-3 has anti-proliferative activity against various cancer cells, inducing G2 phase arrest and apoptosis in liver cancer cells HepG2.
    SphK2-IN-3
  • HY-10493R
    Cobicistat (Standard) 1004316-88-4
    Cobicistat (Standard) is the analytical standard of Cobicistat. This product is intended for research and analytical applications. Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.
    Cobicistat (Standard)
  • HY-167828
    ARN25062 3036492-85-7
    ARN25062 (compound 27) is a CDC42/RHOJ inhibitor with antitumor activity. ARN25062 is a novel trisubstituted pyrimidine derivative.
    ARN25062
  • HY-137389
    Anhydro abiraterone 154229-20-6
    Anhydro abiraterone is a degradation product of Abiraterone acetate (HY-75054). Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity.
    Anhydro abiraterone
  • HY-W244282
    Thalidomide-pinacolborane 2229725-98-6
    Thalidomide-pinacolborane is a Thalidomide analogue featuring a boronic pinacol ester, otherwise known as a Bpin group, and they are most frequently used in Suzuki reactions. This molecule is an activator for E3 ligase, which ubiquitinylates proteins, thus committing their fate to proteolytic destruction.
    Thalidomide-pinacolborane
  • HY-13599S
    Cladribine-d4
    Cladribine-d4 (2-Chloro-2′-deoxyadenosine-d4) is deuterium labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
    Cladribine-d<sub>4</sub>
  • HY-P991132
    Efclarofusp alfa 3053638-35-7
    Efclarofusp alfa is a CHO-expressed humanized antibody consisting of VEGFR-1 and VEGFR-2 regions fused to human IgG1 Fc. Efclarofusp alfa is an angiogenesis inhibitor.
    Efclarofusp alfa
  • HY-15654R
    Sodium 4-phenylbutyrate (Standard) 1716-12-7
    Sodium 4-phenylbutyrate (Standard) is the analytical standard of Sodium 4-phenylbutyrate. This product is intended for research and analytical applications. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
    Sodium 4-phenylbutyrate (Standard)
  • HY-121667
    Scaff10-8 777857-56-4
    Scaff10-8, bound to RhoA, inhibits the AKAP-Lbc-mediated RhoA activation.
    Scaff10-8
  • HY-160235
    Pomalidomide-C2-amide-C5-azide 2732859-29-7
    Pomalidomide-C2-amide-C5-azidea is an E3 linker conjugate, pomalidomide, that can be used to synthesize highly effective PROTAC molecules towards CDK9. Pomalidomide-C2-amide-C5-azidea has antiproliferative activity.
    Pomalidomide-C2-amide-C5-azide
  • HY-10172R
    IMD-0354 (Standard) 978-62-1
    IMD-0354 (Standard) is the analytical standard of IMD-0354. This product is intended for research and analytical applications. IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity[1]. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM[2].
    IMD-0354 (Standard)
  • HY-159909
    ATMW-2
    ATMW-2 is a NeuralGenThesis (NGT)-derived antagonist targeting the melanocortin type 2 receptor (MC2R).
    ATMW-2
  • HY-B0130S
    Perindopril-d4 erbumine 1356929-59-3
    Perindopril-d4 t-butylamine salt is the deuterium labeled Perindopril t-butylamine salt. Perindopril t-butylamine salt is a long-acting ACE inhibitor of which is used to treat high blood pressure, heart failure or stable coronary artery disease.
    Perindopril-d<sub>4</sub> erbumine