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.
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CRBN ligand-758
0 ImagesCat. No.: HY-W953652CAS No.: 2925100-01-0
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Keap1-Nrf2-IN-17
0 ImagesCat. No.: HY-162096CAS No.: 3042821-85-9Keap1-Nrf2-IN-17 (compound 18) is a potent inhibitor of Keap1-Nrf2 protein-protein interaction.
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tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate hydrochloride
![tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate hydrochloride](https://file.medchemexpress.com/product_pic/hy-30590.gif "Click to View tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate hydrochloride Product Detail")
0 ImagesCat. No.: HY-30590CAS No.: 869976-20-5
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GW280264X (Standard)
0 ImagesCat. No.: HY-115670RCAS No.: 866924-39-2GW280264X (Standard) is the analytical standard of GW280264X (HY-115670). This product is intended for research and analytical applications. GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells.
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Y06137 (Standard)
0 ImagesCat. No.: HY-111503RCAS No.: 2226534-49-0Y06137 (Standard) is the analytical standard of Y06137 (HY-111503). This product is intended for research and analytical applications. Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM.
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Erlotinib-d4
0 ImagesCat. No.: HY-50896S2CAS No.: 1130852-41-3Synonyms: CP-358774-d4; NSC 718781-d4; OSI-774-d4Erlotinib-d4 (CP-358774-d4) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions.
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Albocycline K3
0 ImagesCat. No.: HY-N14938CAS No.: 178114-31-3Albocycline K3 is a melanogenesis inhibitor of microbial origin.
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2-(2,6-Dioxopiperidin-3-yl)phthalimidine-O-piperidine
0 ImagesCat. No.: HY-W1112836CAS No.: 2222115-81-1
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CRBN ligand-385
0 ImagesCat. No.: HY-W952808CAS No.: 2925074-79-7
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N,O-Didesmethylvenlafaxine
0 ImagesCat. No.: HY-138818CAS No.: 135308-74-6Synonyms: NODVFXN,O-Didesmethylvenlafaxine (NODVFX) is a metabolite of Venlafaxine (VFX; HY-B0196). Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor.
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Atomoxetine hydrochloride (Standard)
0 ImagesSynonyms: Tomoxetine hydrochloride (Standard); (R)-Tomoxetine hydrochloride (Standard); LY 139603 (Standard)Atomoxetine (hydrochloride) (Standard) is the analytical standard of Atomoxetine (hydrochloride). This product is intended for research and analytical applications. Atomoxetine (Tomoxetine) hydrochloride is a selective noradrenaline reuptake inhibitor with Ki values of 5 nM, 77 nM and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine hydrochloride is a potent Na+ channels (VGSCs) blocker. Atomoxetine hydrochloride can be used for attention-deficit hyperactivity disorder (ADHD) research.
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E7090 (Standard)
0 ImagesCat. No.: HY-101466RCAS No.: 1622204-21-0E7090 (Standard) is the analytical standard of E7090 (HY-101466). This product is intended for research and analytical applications. E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively.
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CRBN ligand-555
0 ImagesCat. No.: HY-W953678CAS No.: 2925099-22-3
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ZYJ-25e
0 ImagesCat. No.: HY-139795CAS No.: 1287261-04-4
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Mardepodect hydrochloride (Standard)
0 ImagesCat. No.: HY-50098ARCAS No.: 2070014-78-5Synonyms: PF-2545920 hydrochloride (Standard)Mardepodect (hydrochloride) (Standard) is the analytical standard of Mardepodect (hydrochloride). This product is intended for research and analytical applications. Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier.
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3,4,5'-Trihydroxy-3'-methoxy-trans-stilbene
0 ImagesCat. No.: HY-N15168CAS No.: 96853-54-23,4,5'-Trihydroxy-3'-methoxy-trans-stilbene (Compound 3) is a stilbenoid compound found in Stuhlmannia moavi. 3,4,5'-Trihydroxy-3'-methoxy-trans-stilbene exerts weak proliferative inhibitory activity and antimalarial activity with IC50 values of 54 and 27 μM against A2780 human ovarian cancer cells and Plasmodium falciparum. 3,4,5'-Trihydroxy-3'-methoxy-trans-stilbene can be used for researches of ovarian cancer and malaria.
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Ponatinib (Standard)
0 ImagesSynonyms: AP24534 (Standard)Ponatinib (Standard) is the analytical standard of Ponatinib. This product is intended for research and analytical applications. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
