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single-agent

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112897

    Autophagy PI3K Apoptosis Cancer
    IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
    IITZ-01
  • HY-16961
    Sitravatinib
    Maximum Cited Publications
    6 Publications Verification

    MGCD516; MG-516

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Inflammation/Immunology Cancer
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
    Sitravatinib
  • HY-15184

    Azalomycin B; Gopalamicin; Efomycin E

    Autophagy Antibiotic Cancer
    Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells .
    Elaiophylin
  • HY-18377

    DR5 Activator

    TNF Receptor Apoptosis Cancer
    Bioymifi (DR5 Activator), a potent TRAIL receptor DR5 activator, binds to the extracellular domain (ECD) of DR5 with a Kd of 1.2 μM. Bioymifi can act as a single agent to induce DR5 clustering and aggregation, leading to apoptosis .
    Bioymifi
  • HY-144670

    Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH3A1-IN-1 (Compound 18) is a potent inhibitor of ALDH3A1 with an IC50 of 1.61 μM. ALDH3A1-IN-1 is more potent than DEAB against patient-derived primary prostate tumor epithelial cells, as single agents or in combination research with docetaxel .
    ALDH3A1-IN-1
  • HY-10025

    Apoptosis Cancer
    (S)-SW IV-52 hydrochloride is a small molecule that can induce apoptosis in ovarian cancer. (S)-SW IV-52 hydrochloride has minimal single-agent activity at concentrations up to 200 μM .
    (S)-SW IV-52 hydrochloride
  • HY-16961A

    MGCD516 malate; MG-516 malate

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Inflammation/Immunology Cancer
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
    Sitravatinib malate
  • HY-145441

    Drug Derivative Cancer
    GEM–IB is the conjugate of gemcitabine (GEM)-5'-phosphate with ibandronate (IB). GEM–IB as a single agent or in combination with Docetaxel (DTX) demonstrates reduced tumor burden, preservation of the bone architecture, and improved the survival in a murine model of osteosarcoma (OS) .
    GEM–IB
  • HY-164461

    Trk Receptor Cancer
    AZD6918 is an orally active and selective Trk tyrosine kinase inhibitor. AZD6918 induces cell death as a single agent and attenuates BDNF/TrkB-induced protection from Etoposide (HY-13629) in vitro. AZD6918 can be used for the research of neuroblastoma .
    AZD6918
  • HY-135805

    EGFR Cancer
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities .
    JBJ-04-125-02
  • HY-103367

    Checkpoint Kinase (Chk) Cancer
    CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer .
    CHK1-IN-7
  • HY-124761

    Polo-like Kinase (PLK) Autophagy Mitosis Cancer
    Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors .
    Poloppin
  • HY-137458

    ARQ 751

    Akt Ser/Thr Protease Cancer
    Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations .
    Vevorisertib
  • HY-122182

    Histone Methyltransferase Apoptosis Cancer
    OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (DOX; HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .
    OTS193320
  • HY-12624
    Narazaciclib
    2 Publications Verification

    ON123300

    CDK AMPK PDGFR Cancer
    Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors . Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM .
    Narazaciclib

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