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Results for "

in vivo preclinical models

" in MedChemExpress (MCE) Product Catalog:

8

Inhibitors & Agonists

2

Fluorescent Dyes

1

Peptides

1

Inhibitory Antibodies

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-147214
    GNE-7883
    5 Publications Verification

    		 YAP Cancer
    GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
    GNE-7883
  • HY-164992
    Trastuzumab vedotin
    2 Publications Verification

    MRG002; Trastuzumab MMAE

    		 Antibody-Drug Conjugates (ADCs) EGFR Microtubule/Tubulin Cancer
    Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma .
    Trastuzumab vedotin
  • HY-13241A
    Ralimetinib
    Maximum Cited Publications
    15 Publications Verification

    LY2228820

    		 p38 MAPK Autophagy Cancer
    Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma .
    Ralimetinib
  • HY-P99852
    Dilpacimab

    ABT165; PR1283233

    		 VEGFR Notch Cancer
    Dilpacimab (ABT165) is a bispecific variable domain immunoglobulin. Dilpacimab binds to and inhibits DLL4 and VEGF and acts as a tumor growth inhibitor. Dilpacimab can be used in research related to metastatic colorectal cancer and advanced solid tumors .
    Dilpacimab
  • HY-P10943
    APO-15

    		Fluorescent Dye Inflammation/Immunology Cancer
    APO-15 is a phosphatidylserine-binding fluorescent probe and apoptosis imaging reagent. APO-15 exhibits high chemical stability under proteolytic and oxidative conditions, enables quantification and imaging of drug-induced apoptosis in preclinical mouse models, and is applicable to fixed tissue samples and multiple in vivo administration routes (Ex = 488 nm; Em = 525 nm). APO-15 can be used in studies related to acute lung injury and breast cancer .
    APO-15
  • HY-12193
    A-349821

    		Histamine Receptor Others
    A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
    A-349821
  • HY-126929
    Trioxacarcin B

    TXN-B

    		 DNA Alkylator/Crosslinker Apoptosis Bacterial Parasite Fungal Infection Cancer
    Trioxacarcin B (TXN-B) is a potent cytotoxic agent and DNA-targeted inhibitor. Trioxacarcin B disrupts DNA function and induces apoptosis in cancer cells. Trioxacarcin B not only effectively inhibits the growth of various Gram-positive and Gram-negative bacteria as well as Plasmodium falciparum, but also blocks the colony formation of cancer stem cells, significantly reduces tumor volume and prolongs survival in preclinical in vivo models. The activity of Trioxacarcin B is highly dependent on its intact spiro-epoxide structure; it loses efficacy once this moiety undergoes hydrolysis, and Trioxacarcin B shows no activity against fungi, microalgae and small RNA viruses. Trioxacarcin B can be used for research on bacterial infections, malaria, and various cancers including colon cancer and melanoma .
    Trioxacarcin B
  • HY-D3186
    HMRef-βGal

    		Fluorescent Dye Glycosidase Cancer
    HMRef-βGal is a fluorescent probe and a substrate responsive to β-galactosidase (β-galactosidase) (Ex/Em=498 nm/505-600 nm). After being cleaved by β-galactosidase, HMRef-βGal triggers significant fluorescence enhancement via intramolecular spirocyclic function regulation. HMRef-βGal generates bright fluorescence in cancer cells with elevated β-galactosidase activity, enabling visualization of tiny peritoneal metastases in mouse models. HMRef-βGal exhibits low in vitro cytotoxicity and low acute in vivo toxicity in mice. HMRef-βGal can be used for preclinical fluorescence-guided diagnosis and cytoreductive surgery of peritoneal metastases, including compatibility with real-time naked-eye detection and endoscopic imaging, as well as for studies related to peritoneal metastases of ovarian cancer .
    HMRef-βGal

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