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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Thalidomide-NH-C10-COOH
0 ImagesCat. No.: HY-130716CAS No.: 2428400-33-1
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AMG-458
0 ImagesAMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively.
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Bromo-PEG2-CH2-Boc
0 ImagesCat. No.: HY-141371CAS No.: 1807518-63-3
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Pruvonertinib
0 ImagesSynonyms: YK-029A
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Br-PEG3-MS
0 ImagesCat. No.: HY-138336CAS No.: 2702323-73-5
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hsa-miR-223-3p antagomir
0 ImagesCat. No.: HY-RI00467Ahsa-miR-223-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
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G7-18NATE TFA
0 ImagesCat. No.: HY-P10224APurity: 98.06%G7-18NATE TFA is a peptide inhibitor of Grb7. G7-18NATE TFA binds to the Grb7-SH2 domain with micromolar affinity (Kd = 18.1 μM). G7-18NATE TFA inhibits cell proliferation, motility, cell invasion and 3D culture formation in several cancer cell lines.
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Pro-GA
0 ImagesCat. No.: HY-171030CAS No.: 2222067-12-9Pro-GA is a γ-glutamyl cyclotransferase (GGCT) inhibitor. Pro-GA inhibits the enzymatic activity of GGCT, disrupts glutathione homeostasis, induces the production of mitochondrial ROS, and upregulates the expression of p21, p27 and p16 in cells. Pro-GA inhibits the growth of cancer cells, induces cell cycle arrest and cellular senescence. Pro-GA exerts anti-tumor effects in breast cancer xenograft mouse models. Pro-GA can be used in research related to bladder cancer and breast cancer.
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Tambiciclib dimaleate
0 ImagesSynonyms: GFH009 dimaleate; JSH-009 dimaleate; SLS009 dimaleateTambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib dimaleate can be used for AML research.
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Pinobanksin
0 ImagesPinobanksin is an antioxidant and anti-ferroptosis agent found in sunflower honey and propolis, with oral activity. Pinobanksin enhances Nrf2-mediated antioxidant defense, inhibits NF-κB inflammation, and suppresses apoptosis and ferroptosis in in vivo models and normal cells. Pinobanksin exhibits apoptosis-inducing effects on B-cell lymphoma cells. Pinobanksin can be used in research related to perfluorooctane sulfonate-induced renal/cardiac toxicity, acute colitis, and B-cell lymphoma.
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Bromo-PEG6-azide
0 ImagesCat. No.: HY-140823CAS No.: 2062663-64-1Bromo-PEG6-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Bromo-PEG6-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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KMG-1068
0 ImagesKMG-1068 is a molecular glue degrader that induces proteasomal degradation of GSPT1 and GSPT2 with DC50 values of 126.7 nM and 42.2 nM, respectively. KMG-1068 binds to the C-terminal IMiD-binding site of CRBN, forms ternary complexes with GSPT1 and GSPT2, and mediates proteasomal degradation of target proteins via the CRL4 ubiquitination pathway. KMG-1068 is applicable to research related to acute myeloid leukemia.
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DBPR728
0 ImagesDBPR728 is an acyl prodrug of 6K465 that carries fewer hydrogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465.
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DP-15
0 ImagesDP-15 is a BRD4 and GSPT1 PROTAC degrader with DC50 values of 0.48 nM and 5.25 nM, respectively. DP-15 induces ubiquitination and degradation of BRD4 and GSPT1. DP-15 induces Apoptosis. DP-15 exerts anticancer activity against acute myeloid leukemia and non-Hodgkin's lymphoma cells. DP-15 can be used in studies related to acute myeloid leukemia and non-Hodgkin's lymphoma.
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DBCO-PEG4-Val-Ala-PAB-PNP
0 ImagesCat. No.: HY-W591374CAS No.: 2348405-93-4DBCO-PEG4-Val-Ala-PAB-PNP is a cleavable ADC linker. The Val-Ala linkers can be cleaved by Cathepsin B. The DBCO groups is commonly used for Click Chemistry reactions. PEG spacer improves the compound's aqueous solubility. PNP is a good leaving group.
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Thalidomide-O-C6-azide
0 ImagesThalidomide-O-C6-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide (HY-14658) based cereblon ligand and a linker used in PROTAC technology. Thalidomide-O-C6-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Biotin-PEG11-azide
0 ImagesBiotin-PEG11-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Biotin-PEG11-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
