store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ribociclib (LEE011) 是一种口服有效的高特异性 CDK4/6 抑制剂,IC50值分别为 10 nM 和 39 nM。
规格 | 价格/CNY | 货期 | 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 * 10 mM (in DMSO) | ¥ 657 | 现货 |
产品描述 | Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor (IC50:10/39 nM). |
靶点活性 | VEGFR6:39 nM, VEGFR4:10nM |
体外活性 | LEE011(200 mg/kg/day,p.o.)明显延缓小鼠中BE2C 或者 1643细胞的生长,且无体重减轻或者其它的毒性症状. |
体内活性 | LEE011可抑制神经细胞瘤细胞的生长,该作用受到G1细胞周期阻滞和细胞衰老的调控。LEE011对17种神经细胞瘤中的12种均有显著的生长抑制作用(平均IC50:307 nM)。 |
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 |
化合物与蛋白结合的复合物 |
The X-ray co-crystal structure of human CDK6 and Ribociclib. |
分子量 | 434.54 |
分子式 | C23H30N8O |
CAS No. | 1211441-98-3 |
store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (115.06 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3013 mL | 11.5064 mL | 23.0128 mL | 57.5321 mL |
5 mM | 0.4603 mL | 2.3013 mL | 4.6026 mL | 11.5064 mL | |
10 mM | 0.2301 mL | 1.1506 mL | 2.3013 mL | 5.7532 mL | |
20 mM | 0.1151 mL | 0.5753 mL | 1.1506 mL | 2.8766 mL | |
50 mM | 0.046 mL | 0.2301 mL | 0.4603 mL | 1.1506 mL | |
100 mM | 0.023 mL | 0.1151 mL | 0.2301 mL | 0.5753 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ribociclib 1211441-98-3 Angiogenesis Cell Cycle/Checkpoint Tyrosine Kinase/Adaptors VEGFR CDK Cyclin dependent kinase 瑞博西尼 inhibit Inhibitor LEE 011 LEE011 LEE-011 inhibitor