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orthotopic xenograft

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12401A
    Mps1-IN-3 hydrochloride
    1 Publications Verification

    		 Mps1 Cancer
    Mps1-IN-3 hydrochloride is a potent and selective Mps1 inhibitor with an IC50 value of 50 nM. Mps1-IN-3 hydrochloride can inhibit the proliferation of glioblastoma cells, and effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft model .
    Mps1-IN-3 hydrochloride
  • HY-143411
    GEM144

    		HDAC Apoptosis DNA/RNA Synthesis Cancer
    GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts .
    GEM144
  • HY-148409
    MMRi62

    		Ferroptosis Apoptosis Autophagy MDM-2/p53 Cancer
    MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
    MMRi62
  • HY-168555
    YJ1206

    		CDK PROTACs Apoptosis Cancer
    YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .
    YJ1206
  • HY-139418
    PX20350

    		FXR Cancer
    PX20350 is a FXR agonist with EC50s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models .
    PX20350
  • HY-178777
    BCL6-760

    		BCL6 Cancer
    BCL6-760 is an orally active BCL-6 PROTAC degrader with an EC50 of 0.8 nM. BCL6-760 only degrades BCL6 and has no effect on other CRBN substrates. BCL6-760 demonstrates significant efficacy in the orthotopic xenograft mouse model of OCI-LY-1 tumors. BCL6-760 can be used in the research of diffuse Large B-cell Lymphoma (DLBCL) (Pink: BCL-6 ligand (HY-179317); Blue: CRBN ligand (HY-179305); Black: Linker) .
    BCL6-760
  • HY-162494
    PAD4-IN-4

    		Protein Arginine Deiminase Cancer
    PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC50=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research .
    PAD4-IN-4
  • HY-163434
    PRMT5/EGFR-IN-1

    		EGFR Histone Methyltransferase Cancer
    PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
    PRMT5/EGFR-IN-1
  • HY-13654
    IPI-269609

    		Smo Hedgehog Cancer
    IPI-269609 is an orally effective Smoothed (SMO) inhibitor that targets the Hedgehog (Hh) signaling pathway. IPI-269609 specifically reduces the ALDH-bright (high aldehyde dehydrogenase activity) cell subset, which is considered the "cancer stem cells" in pancreatic cancer. IPI-269609 significantly inhibits the migration and colony formation of pancreatic cancer cells. IPI-269609 effectively inhibits pancreatic cancer metastasis in a mouse model. IPI-269609 can be used for pancreatic cancer research .
    IPI-269609

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