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-W070753
    LIMK1 inhibitor 2 67795-42-0
    LIMK1 inhibitor 2 (compound 41) is a LIMK1 inhibitor with the IC50 of 9 μM.
    LIMK1 inhibitor 2
  • HY-W800624
    Boc-PEG2-Val-Cit-PAB-OH 2055024-55-8
    Boc-PEG2-Val-Cit-PAB-OH is an enzyme-cleavable ADC linker featuring a Boc-protected amine, a hydrophilic PEG spacer, and a Val-Cit-PAB dipeptide. The benzylic alcohol on the PAB can be used to attach with reactive groups such as PNP for conjugation with drug payloads. The Boc protecting group may be removed with acid to reveal a primary amine which may be used in coupling reactions to form amides. The Val-Cit-PAB is cleaved by cellular proteases for efficient release of payloads to the cell.
    Boc-PEG2-Val-Cit-PAB-OH
  • HY-N0370R
    Bergapten (Standard) 484-20-8
    Bergapten (Standard) is the analytical standard of Bergapten. This product is intended for research and analytical applications. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
    Bergapten (Standard)
  • HY-B0161S3
    Duloxetine-d5 oxalate 1276197-53-5
    Duloxetine-d5 (oxalate) ((S)-Duloxetine-d5 (oxalate)) is deuterium labeled Duloxetine. Duloxetine is a serotonin-norepinephrine reuptake inhibitor with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).
    Duloxetine-d<sub>5</sub> oxalate
  • HY-16379R
    Pacritinib (Standard) 937272-79-2
    Pacritinib (Standard) is the analytical standard of Pacritinib. This product is intended for research and analytical applications. Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).
    Pacritinib (Standard)
  • HY-157647
    1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC 137254-39-8
    1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) is an inhibitor of cyclin-dependent kinases (CDKs).? 1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC induces apoptosis and inhibits the growth of various cancer cell lines.
    1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC
  • HY-119818
    Farnesylthiotriazole 156604-45-4
    Farnesylthiotriazole (FTT) is a PKC activator (Kd=0.8 μM) that can be used in cancer research.
    Farnesylthiotriazole
  • HY-18282R
    AZ876 (Standard) 898800-26-5
    AZ876 (Standard) is the analytical standard of AZ876. This product is intended for research and analytical applications. AZ876 is a selective, orally active agonist of liver X receptor (LXRα/β) (Ki=0.007 μM [LXRα, human], 0.011 μM [LXRβ, human]. AZ876 induces the expression of target genes such as ABCA1 and ABCG1, promotes reverse cholesterol transport (RCT) and regulates lipid metabolism and anti-inflammatory effects. AZ876 increases cardiac polyunsaturated fatty acid levels, reduces myocardial fibrosis, and reduces lesion area and monocyte adhesion in atherosclerosis models. AZ876 can be used in cardiovascular disease research, such as preventing and treating β-adrenergic-induced cardiac diastolic dysfunction and inhibiting the progression of atherosclerosis.
    AZ876 (Standard)
  • HY-133838
    Ilmofosine 83519-04-4
    Ilmofosine (BM41440) is a potent and selective protein kinase C inhibitor. Ilmofosine induces cell cycle arrest at the G2 phase. Ilmofosine also is an anti-leishmanial agent.
    Ilmofosine
  • HY-B0656R
    Rabeprazole (Standard) 117976-89-3
    Rabeprazole (Standard) is the analytical standard of Rabeprazole. This product is intended for research and analytical applications. 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 (Standard)
  • HY-155209
    SCD1 inhibitor-5 1673558-59-2
    SCD1 inhibitor-5 (compound 51) is a SCD1 inhibitor,with the IC50 values​ of 0.13 μM and 31 μM for H2122 and H1819, respectively. SCD1 inhibitor-5 can be used in cancer research.
    SCD1 inhibitor-5
  • HY-171442A
    (R)-PIN1 ligand-2
    (R)-PIN1 ligand-2 is a PIN1 ligand, and can be used for synthesis of PROTACs, such as P1D-34 (HY-171334A).
    (R)-PIN1 ligand-2
  • HY-156310
    BCN-endo-PEG7-NH2 2143968-34-5
    BCN-endo-PEG7-NH2 is an ADC Linker containing 7 PEG units. BCN-endo-PEG7-NH2 contains the lyophilic bidentate macrocyclic ligand endo-BCN, which can further synthesize macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
    BCN-endo-PEG7-NH2
  • HY-133380
    DSPE-PEG36-mal
    DSPE-PEG36-mal is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    DSPE-PEG36-mal
  • HY-156069
    Methylspinazarin 41768-12-1
    Methylspinazarin is a potent inhibitor of catechol O-methyltransferase (COMT, IC50 = 0.8 μg/ml) that can be isolated from Streptomyces. Methylspinazarin is selective for COMT over tyrosine hydroxylase.
    Methylspinazarin
  • HY-128067R
    5-(N,N-Hexamethylene)-amiloride (Standard) 1428-95-1
    5-(N,N-Hexamethylene)-amiloride (Standard) is the analytical standard of 5-(N,N-Hexamethylene)-amiloride. This product is intended for research and analytical applications. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.
    5-(N,N-Hexamethylene)-amiloride (Standard)
  • HY-15493
    AN-019 879507-25-2
    AN-019 is a Bcr-Abl kinase inhibitor. AN-019 has antitumor activity.
    AN-019
  • HY-101775AR
    9-Hydroxyellipticine hydrochloride (Standard) 52238-35-4
    9-Hydroxyellipticine (hydrochloride) (Standard) is the analytical standard of 9-Hydroxyellipticine (hydrochloride). This product is intended for research and analytical applications. 9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC50 values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively.
    9-Hydroxyellipticine hydrochloride (Standard)
  • HY-32718R
    Pelitinib (Standard) 257933-82-7
    Pelitinib (Standard) is the analytical standard of Pelitinib. This product is intended for research and analytical applications. Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
    Pelitinib (Standard)
  • HY-77324S
    4-(Trifluoromethyl)aniline-d4 1219795-48-8 99.23%
    4-(Trifluoromethyl)aniline-d4 is deuterium labeled 4-(Trifluoromethyl)aniline. 4-(Trifluoromethyl)aniline is a DYRK1A and DYRK1B kinase inhibitor with IC50s of 54.84 nM and 186.40 nM, respectively.
    4-(Trifluoromethyl)aniline-d<sub>4</sub>