LEE011 succinate,1374639-75-4_详细资料

产品信息

货号： abs814339 CAS号： 1374639-75-4 供应商：爱必信(上海) 生物科技有限公司数量： 99 英文名： Ribociclib; LEE 011; LEE-011 保质期：见爱必信官网保存条件： store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 规格： 100mg

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YZ剂描述：
产品名称：LEE011 succinate
产品别名：Ribociclib; LEE 011; LEE-011
英文别名：Ribociclib;LEE 011;LEE-011
靶点：CDK
CAS：1374639-75-4
纯度：>98%
外观：Powder
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.
描述：LEE011 succinate is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.
溶解性：
In Vitro:
DMSO : 62.5 mg/mL (113.10 mM; Need ultrasonic)
Preparing
Stock Solutions
ConcentrationSolventMass 1 mg 5 mg 10 mg
1 mM 1.8095 mL 9.0476 mL 18.0953 mL
5 mM 0.3619 mL 1.8095 mL 3.6191 mL
10 mM 0.1810 mL 0.9048 mL 1.8095 mL
*请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存方式和期限。
In Vivo:
请根据您的实验动物和给YF式选择适当的溶解方案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的工作
液，建议您现用现配，当天使用；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分比是指该溶剂在您配制终溶液中的体积占比)：
1.
请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline
Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution
2.
请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution
*
体外研究：
Treating a panel of 17 neuroblastoma cell lines with Ribociclib (LEE011) across a four-log dose range (10 to 10,000 nM). Treatment with Ribociclib significantly inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC₅₀=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC₅₀ of less than 1 μM. Ribociclib treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition results in a dose-dependent accumulation of cells in the G₀/G₁ phase of the cell cycle. This G₀/G₁ arrest becomes significant at Ribociclib concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively.
体内研究：
CB17 immunodeficient mice bearing BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts are treated once daily for 21 days with Ribociclib (LEE011; 200 mg/kg) or with a vehicle control. This dosing strategy is well tolerated, as no weight loss or other signs of toxicity are observed in any of the xenograft models. Tumor growth is significantly delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment.
产品信息订购：

  产品货号   产品名称   规格价格大包装及货期

  abs814339   LEE011 succinate   100mg   5850   立即咨询

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