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Ribociclib

产品编号 T6199Cas号 1211441-98-3
别名 瑞博西尼, LEE011

Ribociclib (LEE011) 是一种细胞周期蛋白依赖性激酶 CDK4/6 抑制剂 (IC50=10/39 nM),具有特异性和口服活性。Ribociclib 具有抗肿瘤活性,可以阻滞细胞周期,抑制肿瘤细胞增殖。

Ribociclib

Ribociclib

纯度: 99.96%
产品编号 T6199 别名 瑞博西尼, LEE011Cas号 1211441-98-3

Ribociclib (LEE011) 是一种细胞周期蛋白依赖性激酶 CDK4/6 抑制剂 (IC50=10/39 nM),具有特异性和口服活性。Ribociclib 具有抗肿瘤活性,可以阻滞细胞周期,抑制肿瘤细胞增殖。

规格价格库存数量
1 mg¥ 233现货
2 mg¥ 329现货
5 mg¥ 535现货
10 mg¥ 828现货
25 mg¥ 1,490现货
50 mg¥ 1,980现货
100 mg¥ 3,450现货
500 mg¥ 5,350现货
1 mL x 10 mM (in DMSO)¥ 657现货
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纯度:99.96%
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产品介绍

生物活性
产品描述
Ribociclib (LEE011) is a cell cycle protein-dependent kinase CDK4/6 inhibitor (IC50 = 10/39 nM) with specific and oral activity. Ribociclib has antitumor activity that blocks the cell cycle and inhibits tumor cell proliferation.
靶点活性
VEGFR4:10nM, VEGFR6:39 nM
体外活性
方法:人乳腺癌细胞 MDA-MB-231 用 Ribociclib (0-20 µM) 处理 24-144 h,使用 CCK8 assay 检测细胞活力。
结果:Ribociclib 抑制 MDA-MB-231 中的细胞增殖。[1]
方法:神经母细胞瘤细胞系 BE2C、IMR5、EBC1 和 SKNAS 用 Ribociclib (0.01-10 µM) 处理 96 h,使用 Western Blot 检测靶点蛋白表达水平。
结果:在 BE2C 和 IMR5 细胞系中,从 250 nM 开始观察到 pRBS780 的耗竭。在 EBC1 和 SKNAS 抗性细胞系中也观察到 pRBS780 的降低,但仅在较高的抑制剂浓度下。[2]
体内活性
方法:为测试体内抗肿瘤活性,将 Ribociclib (200 mg/kg in 0.5 % methylcellulose) 口服给药给携带神经母细胞瘤 BE2C、NB-1643 或 EBC1 的 CB17 小鼠,每天一次,持续二十一天。
结果:在携带 BE2C 或 1643 异种移植物的小鼠中,肿瘤生长在整个 21 天的治疗过程中显著延迟。在 EBC1 异种移植物模型中,肿瘤生长抑制不那么有力。[2]
激酶实验
Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70[1].
细胞实验
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 are analyzed using a nonlinear log inhibitor versus normalized response function. All experiments are repeated at least once. (Only for Reference)
别名瑞博西尼, LEE011
化学信息
分子量434.54
分子式C23H30N8O
CAS No.1211441-98-3
储存&溶解度
存储store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 50 mg/mL (115.06 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.51 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
10% DMSO+40% PEG300+5% Tween 80+45% Saline/DMSO
1mg5mg10mg50mg
1 mM2.3013 mL11.5064 mL23.0128 mL115.0642 mL
5 mM0.4603 mL2.3013 mL4.6026 mL23.0128 mL
10 mM0.2301 mL1.1506 mL2.3013 mL11.5064 mL
DMSO
1mg5mg10mg50mg
20 mM0.1151 mL0.5753 mL1.1506 mL5.7532 mL
50 mM0.0460 mL0.2301 mL0.4603 mL2.3013 mL
100 mM0.0230 mL0.1151 mL0.2301 mL1.1506 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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