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  • OSU-03012
    • OSU03012;AR-12
    货号: abs813248
    CAS号: 742112-33-0
    分子式: C26H19F3N4O
    分子量: 460.45
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs813248-10mg 1-2周 ¥1077.00
    - +
    abs813248-25mg 1-2周 ¥1726.00
    - +
    abs813248-50mg 1-2周 ¥3260.00
    - +
    abs813248-100mg 1-2周 ¥5855.00
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    大包装询价
    产品描述
    描述

    OSU-03012 (AR-12)是一种有效的重组PDK-1抑制剂,IC50为5 μM,比OSU-02067作用效果高2倍。OSU-03012诱导PC-3细胞凋亡,IC50为5 µM,且降低免疫沉淀的p70S6K的活性。Celecoxib完全抑制肿瘤细胞生长,浓度至少需要50 μM,而OSU-03012浓度为3-5 μM时即可完全抑制多种肿瘤细胞生长。 与作用于正常的胶质细胞相比,OSU-03012作用于神经胶质瘤细胞更有效促进细胞死亡。

    纯度
    >98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    OSU03012;AR-12
    可溶性/溶解性
    DMSO :9 mg/mL (19.5 mM)
    生物活性
    靶点
    PDK-1
    In vitro(体外研究)
    OSU-03012 induces apoptotic death in PC-3 cells with IC50 of 5 µM and reduces the activity of immunoprecipitated p70S6K. OSU-03012 completely suppress cell growth in a diverse range of tumor cell lines at concentrations of 3–5 μm, as compared with the concentration of at least 50 μm required for celecoxib. OSU-03012 promotes cell killing to a greater extent in glioma cells than in nontransformed astrocytes. OSU-03012 causes a dose-dependent induction of cell death that is not altered by p53 mutation, expression of ERBB1 VIII, or loss of phosphatase and tensin function due to a homolog deletion on chromosome 10. OSU-03012 and ionizing radiation cause an additive, caspase-independent elevation in cell killing. OSU-03012 lethality as a single agent or when combined with signaling modulators is not modified in cells lacking expression of BIM or of BAX/BAK. OSU-03012 promotes the release of cathepsin B from the lysosomal compartment and that of AIF from mitochondria. The lethality of OSU-03012 is attenuated in protein kinase R-like endoplasmic reticulum kinase-/- cells, which correlated with the reduced cleavage of BID and suppression of cathepsin B and AIF release into the cytosol. OSU-03012 inhibits thyroid cancer cell (NPA, WRO, and ARO cells) proliferation, migration and induces apoptosis, which results in an increase of cells in the S phase without an increase of cells in G2. OSU-03012 is an ATP-competitive inhibitor of PAK activity and suppresses the phosphorylation of AKT in thyroid cancer cells. OSU-03012 inhibits cell growth of hepatocellular carcinoma cell lines including Huh7, Hep3B and HepG2 cells with IC50 values below 1 μM. OSU-03012 does not suppress PDK1 or AKT activity or induce cellular apoptosis but induces autophagy in Huh7 cells. Moreover, accumulation of reactive oxygen species (ROS) is detected after OSU-03012 treatment. A recent study shows that OSU-03012 could enhance the susceptibility of (Bcr)-Abl mutant cell lines to imatinib-induced apoptosis.
    In vivo(体内研究)
    OSU-03012 suppresses tumor growth by 57.59% and increases cleaved LC3 in Huh7 tumor xenografts at 200 mg/kg. OSU-03012 remarkably decreases expression of EGFR protein in the tumors by 48% compared with vehicle controls and also prevents YB-1 from binding to the EGFR promoter in MDA-MB-435/LCC6 xenografts. OSU-03012 is well tolerated and inhibits the growth of HMS-97 schwannoma xenografts by 55% after oral administration.
    参考文献
    参考文献
    OSU-03012 suppresses GRP78/BiP expression that causes PERK-dependent increases in tumor cell killing.
    Booth et al. Cancer Biol Ther. 2012 Feb 15;13(4):224-36. PMID: 22354011.
    Endogenous adenosine contributes to renal sympathetic neurotransmission via postjunctional A1 receptor-mediated coincident signaling.
    Jackson et al. Am J Physiol Renal Physiol. 2012 Feb;302(4):F466-76. PMID: 22114202.
    The phosphoinositide-3-kinase-Akt signaling pathway is important for Staphylococcus aureus internalization by endothelial cells.
    Oviedo-Boyso et al. Infect Immun. 2011 Nov;79(11):4569-77. PMID: 21844240.
    OSU-03012, a novel celecoxib derivative, induces cell swelling and shortens action potential duration in mouse ventricular cells.
    Yamamoto et al. Biomed Res. 2010 Dec;31(6):413-7. PMID: 21187652.
    OSU-03012 enhances Ad.7-induced GBM cell killing via ER stress and autophagy and by decreasing expression of mitochondrial protective proteins.
    Hamed et al. Cancer Biol Ther. 2010 Apr;9(7):526-36. PMID: 20107314.
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
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