全部分类
  • CRT0066101 dihydrochloride
CRT0066101 dihydrochloride的可视化放大

CRT0066101 dihydrochloride

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

此产品仅用于科学研究,我们不为任何个人用途提供产品和服务

CRT0066101 dihydrochloride的二维码
  • 库存: 现货
可选规格
  • 包装
    价格
    促销价
    数量
  • 5mg
    ¥887.00
    710.00
    - +
  • 10mg
    ¥1625.00
    1300.00
    - +
  • 25mg
    ¥3662.00
    2930.00
    - +
  • 50mg
    ¥6587.00
    5270.00
    - +
  • 100mg
    ¥0.00
    0.00
    - +
  • 200mg
    ¥0.00
    0.00
    - +
已选 0 0
金额: ¥0.00
首页 收藏
  • 货号: ajce55742
  • CAS: 1883545-60-5
  • 别名:
  • 分子式: C18H23ClN6O
  • 分子量: 374.87
  • 纯度: >98%
  • 溶解度: Water: 50 mg/mL (133.38 mM); DMSO: ≥ 25 mg/mL (66.69 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

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


CRT0066101 reduces BrdU incorporation, increases apoptosis, blocks neurotensin (NT)-induced PKD1/2 activation, reduces NT-induced PKD-mediated Hsp27 phosphorylation, attenuates PKD1-mediated NF-κB activation, and abrogates expression of NF-κB-dependent-dependent proliferative and pro-survival proteins. CRT0066101 significantly inhibits Panc-1 cell proliferation with an IC50 value of 1 μM. It also significantly reduces cell proliferation of Colo357, Panc-1, MiaPaCa-2, and AsPC-1 cells but has a modest effect in Capan-2 cells. Thus, CRT0066101 significantly blocks proliferation of PaCa cells that express moderate to high endogenous levels of PKD1/2. CRT0066101 (5 ?M) blocks both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells, also abrogates NT-induced phosphorylation of Hsp27 (pS82-Hsp27), which is a physiological substrate of PKD1/2 in a dose-dependent manner[1].


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 ?M) of CRT0066101 achieved within 2 h after oral administration. 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 (p< 0.01), increases TUNEL+ apoptotic cells (p<0.05), and abrogates expression of NF-κB-dependent proteins including cyclin D1, survivin, and cIAP-1. CRT0066101 blocks Panc-1 cell proliferation and growth in multiple xenograft models[1]


[1] Harikumar KB, et al. Mol Cancer Ther. 2010, 9(5):1136-46. [2] Miyamoto K, et al. Int Immunol. 2022 Jul 16:dxac035.

没有评价数据

温馨提示 ×
商品已成功加入购物车!
购物车共 0 件商品
去购物车结算