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当前位置: 首页 > 信号通路研究 > Gamma-secretase > LY3039478
LY3039478
LY3039478
LY3039478
商品货号:MB3802
CAS 号:1421438-81-4
英文名字:LY3039478
质量标准:>98%,BR
分子式:C22H23F3N4O4
  • 包装规格:
    规格 库存 发货时间
    5MG [¥980.00]15 现货一周内发货
    25MG [¥2800.00]15 现货一周内发货
  • 购买数量:
  • 会员尊享价:

    商品信息

    质检证书(coa)

    说明书下载

    LY3039478是一种有效的Notch抑制剂,IC50为0.41 nM。

    理化数据

    分子量

    464.44

    化学式

    C22H23F3N4O4

    CAS

    1421438-81-4

    稳定性

    3 years -20°C powder

    溶解性

    DMSO

    92 mg/mL (198.08 mM)

    Ethanol

    71 mg/mL (152.87 mM)

    Water

    Insoluble

    生物活性

    产品描述

    LY3039478是一种有效的Notch抑制剂,IC50为0.41 nM。

    靶点

    Notch-1

    ~1 nM

    体外研究

    LY3039478 is a novel small molecule that is an exquisitely potent inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with an IC50 of ∼1nM in most of the tumor cell lines tested. LY3039478 also potently inhibits mutant Notch receptor activity. Treatment with a gamma secretase inhibitor, LY3039478, significantly inhibited the growth of 2 CCRCC(Clear cell renal cell carcinoma) cell lines in a concentration dependent manner. LY3039478 treatment also led to decreased expression of Myc and Cyclin A1, two genes that were part of the NOTCH driven proliferative signature in murine and human model systems. LY3039478 treatment also led to G0/G1 cell cycle arrest in CCRCC cells。

    体内研究

    In mice, its oral bioavalability(%F) is 65%, clearance(CL)=41 mL/min/kg, VDss = 3.8 L/kg. In Rats, its oral bioavalability(%F) is 65%, CL=98 mL/min/kg, VDss=4.9 L/kg. In Dogs, its oral bioavalability (%F) is 67%, CL=3.8 mL/min/kg, VDss=1.4 L/kg. In a xenograft tumor model, LY3039478 inhibited N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment. The inhibition of Notch cleavage also resulted in the induction of apoptosis in a Notch-dependent xenograft model. In immunodeficient NSG mice xenografted with 769-P CCRCC cells, LY3039478 treatment resulted in significantly increased survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC。

    实验操作

    细胞实验:
    • Cell lines: K07074 cells
    • Concentrations: 100 nM
    • Incubation Time: 24, 48, 72, 96 h
    • Method: K07074 cells were plated to 24-well plates at 10<sup>5</sup> cell/well. Viability of cells was assessed in quadruplicates at indicated timepoints using the CellTiter-Glo luminescent cell viability assay. To study the effect of the small molecular compounds on K07074 cell growth the compounds or DMSO were added to the growth media 24 h after seeding. The cells were incubated with inhibitors and DMSO as indicated. Cell viability was assessed as described above. Each experiment was carried out in triplicate and at least 3 independent experiments were performed

    动物实验:

    • Animal Models: Mice
    • Formulation: 1% Na-CMC, 0.25% Tween-80 and 0.05% anti-foam
    • Dosages: 8 mg/kg
    • Administration: oral gavage
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