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Ribociclib

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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

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纯度: 100%
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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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
VEGFR6:39 nM, VEGFR4:10nM
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
SmilesC(N(C)C)(=O)C=1N(C=2C(C1)=CN=C(NC3=CC=C(C=N3)N4CCNCC4)N2)C5CCCC5
密度1.39 g/cm3 (Predicted)
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), In vivo: 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
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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