貨號	規(guī)格	價格	上海	北京	武漢	南京
S82374-5mg	99.8%	￥571.00 S82374-5mg ￥571.00 現(xiàn)貨	290 >10	-	-	-
S82374-10mg	99.8%	￥693.60 S82374-10mg ￥693.60 現(xiàn)貨	150 >10	-	-	-
S82374-50mg	99.8%	￥2652.00 S82374-50mg ￥2652.00 現(xiàn)貨	36 >10	-	-	-
S82374-100mg	99.8%	￥3400.00 S82374-100mg ￥3400.00 現(xiàn)貨	23 >10	-	-	-

產(chǎn)品介紹

Ribociclib (LEE011) hydrochloride 是一種高度特異性的針對 CDK4 和 CDK6 的雙重抑制劑，對應的IC50值分別為10 nM和39 nM

產(chǎn)品描述：

Ribociclib (LEE011) hydrochloride 是一種高度特異性的針對 CDK4 和 CDK6 的雙重抑制劑，對應的IC50值分別為10 nM和39 nM

靶點：

CDK4(Cell-free assay):10 nM; CDK6(Cell-free assay):39 nM;CDK

體外研究：

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.

體內(nèi)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.

細胞實驗：

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

動物實驗：

Animal Models: Mice bearing BE2C, NB-1643, or EBC1 xenografts Dosages: ~200 mg/kg daily Administration: p.o.

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻

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LEE011 (hydrochloride)