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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1,4-Di(3-hydroxypropoxy)butane
0 ImagesCat. No.: HY-W442085CAS No.: 2052305-98-1
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Mal-amido-PEG8-C2-acid (Standard)
0 ImagesCat. No.: HY-101159RCAS No.: 1334177-86-4Mal-amido-PEG8-C2-acid (Standard) is the analytical standard of Mal-amido-PEG8-C2-acid (HY-101159). This product is intended for research and analytical applications. Mal-amido-PEG8-C2-acid (example 142) is a nonclaevable ADC linker.
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CDK8-IN-16
0 ImagesCat. No.: HY-171174CAS No.: 1860885-61-5CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%.
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Heptacosanedioic Acid
0 ImagesCat. No.: HY-W674306CAS No.: 5638-06-2
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BRPF1B/TRIM24-IN-1
0 ImagesCat. No.: HY-122626CAS No.: 1242907-48-7BRPF1B/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.
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Laduviglusib monohydrochloride (Standard)
0 ImagesSynonyms: CHIR-99021 monohydrochloride (Standard); CT99021 monohydrochloride (Standard)Laduviglusib (monohydrochloride) (Standard) is the analytical standard of Laduviglusib (monohydrochloride). This product is intended for research and analytical applications. Laduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy.
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EAI001 (Standard)
0 ImagesCat. No.: HY-100214RCAS No.: 892772-75-7EAI001 (Standard) is the analytical standard of EAI001 (HY-100214). This product is intended for research and analytical applications. EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer.
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Elobixibat (Standard)
0 ImagesSynonyms: A 3309 (Standard); AZD 7806 (Standard)Elobixibat (Standard) is the analytical standard of Elobixibat (HY-15790). This product is intended for research and analytical applications. Elobixibat (A 3309; AZD 7806) is orally active, bile acid transporter (IBAT) inhibitor with IC50 values ??of 0.53 nM (human IBAT), 0.13 nM (mouse IBAT), and 5.8 nM (canine IBAT). Elobixibat can lower LDL cholesterol, increase serum GLP-1, promote colonic motility, and has the potential to treat metabolic syndrome. Elobixibat can be used in the study of chronic functional constipation (CIC), dyslipidemia, non-alcoholic hepatitis, and liver tumors in the elderly.
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(R)-Elsubrutinib (Standard)
0 ImagesCat. No.: HY-109143BRCAS No.: 1643570-23-3Synonyms: (R)-ABBV-105 (Standard)(R)-Elsubrutinib (Standard) is the analytical standard of (R)-Elsubrutinib (HY-109143B). This product is intended for research and analytical applications. (R)-Elsubrutinib ((R)-ABBV-105) is a Btk inhibitor. (R)-Elsubrutinib can be used in studies of immune diseases (such as rheumatoid arthritis, psoriasis, ankylosing spondylitis, asthma, systemic lupus erythematosus) and cancer.
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2-Nonylimidazole
0 ImagesCat. No.: HY-184861CAS No.: 52819-56-42-Nonylimidazole is a CYP2A13 inhibitor with an IC50 of 277 μM. 2-Nonylimidazole modulates the enzymatic activity of CYP2A13. 2-Nonylimidazole is applicable to research on drug metabolism and tobacco-related cancers.
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CRBN ligand-739
0 ImagesCat. No.: HY-W953509CAS No.: 2925093-80-5
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TPOP146 (Standard)
0 ImagesCat. No.: HY-100697RCAS No.: 2018300-62-2
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CRBN ligand-84
0 ImagesCat. No.: HY-170131CAS No.: 3065251-76-2
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CRBN ligand-408
0 ImagesCat. No.: HY-W455176CAS No.: 2152673-38-4
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Taltobulin intermediate-11
0 ImagesCat. No.: HY-46005CAS No.: 1822561-77-2Taltobulin intermediate-11 is an intermediate in the synthesis of Taltobulin (HY-15584). Taltobulin is a common toxin component in ADC preparation (ADC Cytotoxin), and it is also a powerful tubulin (Microtubule/Tubulin) inhibitor. Taltobulin disrupts tubulin polymerization, induces mitotic arrest, and induces apoptosis.
