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  • CRT0066101 dihydrochloride

    • CRT0066101
    货号: abs811981
    CAS号: 1883545-60-5
    分子式: C18H22N6O.2HCl
    分子量: 411.33
    产品说明书
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    货号-规格 货期 价格 数量
    abs811981-5mg 1-2周 ¥994.00
    - +
    abs811981-25mg 1-2周 ¥4123.00
    - +
    大包装询价
    产品描述
    描述

    CRT0066101 is a small molecule PKD family specific inhibitor which specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple. 

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    CRT0066101
    外观
    powder
    可溶性/溶解性
    DMSO :25 mg/mL (60.78 mM)

    Water :82 mg/mL (199.35 mM)
    生物活性
    靶点
    PKD1,PKD2,PKD3
    In vitro(体外研究)
    CRT0066101 specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple cancer cell types including A549 (lung) and MiaPaCa-2 (pancreas). CRT0066101 significantly inhibits Panc-1 cell proliferation with an IC50 value of 1 µM. Treatment with CRT0066101 results in a 6-10 fold induction of apoptosis in Panc-1 cells. CRT0066101 significantly reduces cell proliferation of Colo357, Panc-1, MiaPaCa-2, and AsPC-1 cells but has a modest effect in Capan-2 cells. CRT0066101 (5 µM) blocks both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells. CRT0066101 reduces PKD-dependent NF-κB activation and NF-κB-dependent gene expressions in Panc-1.
    In vivo(体内研究)
    Optimal therapeutic concentrations (8 µM) of CRT0066101 are detectable 6 h after oral administration of this drug. CRT0066101 given orally (80 mg/kg/day) for 28 days significantly abrogates PaCa growth in Panc-1 subcutaneous xenograft model. Activated PKD1/2 expression in the treated tumor-explants is significantly inhibited with peak tumor concentration (12 µM) of CRT0066101 achieved within 2 h after oral administration. Further, CRT0066101 given orally (80 mg/kg/day) for 21 days in Panc-1 orthotopic model potently blocks tumor growth in vivo. CRT0066101 significantly reduces Ki-67+ proliferation index, increases TUNEL+ apoptotic cells (p<0.05), and abrogates expression of NF-κB-dependent proteins including cyclin D1, survivin, and cIAP-1.
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
    • 实验方法 实验条件
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