| 产品描述： | Ribociclib (LEE011) hydrochloride 是一种高度特异性的针对 CDK4 和 CDK6 的双重抑制剂，对应的IC50值分别为10 nM和39 nM |
| 靶点： |
CDK4(Cell-free assay):10 nM; CDK6(Cell-free assay):39 nM;CDK |
| 体外研究： |
LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is mediated by a G1 cell-cycle arrest and cellular senescence. |
| 体内研究： |
LEE011 (200 mg/kg daily, p.o.) significantly causes tumor growth delay in mice harboring the BE2C or 1643 xenografts with no weight loss or other signs of toxicity. |
| 细胞实验： |
Cell lines: BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1 cell lines Concentrations: 10 μM Incubation Time: ~100 h Method: A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, is plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system and treated 24 hours later with a four-log dose range of inhibitor or with a dimethyl sulfoxide (DMSO) control. Cell indexes are monitored continuously for ~100 hours, and IC50 values are determined as follows: growth curves are generated by plotting the cell index as a function of time and are normalized to the cell index at the time of treatment for a baseline cell index of 1. The area under the normalized growth curve from the time of treatment to 96 hours posttreatment is then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas are normalized to the DMSO control, and the resulting data ar |
| 动物实验： |
Animal Models: Mice bearing BE2C, NB-1643, or EBC1 xenografts Dosages: ~200 mg/kg daily Administration: p.o. |
| 参考文献： |
1. Todd VanArsdale, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10. 2. Rader J, et al. Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013, 19(22), 6173-6182. |
| 溶解性： |
Soluble in DMSO、H2O、Ethanol |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.123 ml |
10.616 ml |
21.232 ml |
| 5 mM |
0.425 ml |
2.123 ml |
4.246 ml |
| 10 mM |
0.212 ml |
1.062 ml |
2.123 ml |
| 50 mM |
0.042 ml |
0.212 ml |
0.425 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京