Ribociclib
别名: LEE011 中文名称：瑞博西利，瑞博西林
Ribociclib是一种可口服的，高度特异性CDK4/6抑制剂。
Ribociclib Chemical Structure
CAS: 1211441-98-3
产品质控
批次：
纯度：
99.99%
99.99
Ribociclib相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| LP8 | Growth Inhibition Assay | 3.33 μM | 24 h | decreases the proportion of cells in S phase | 25028469 |
| LP6 | Growth Inhibition Assay | 3.33 μM | 24 h | decreases the proportion of cells in S phase | 25028469 |
| LP3 | Growth Inhibition Assay | 3.33 μM | 24 h | decreases the proportion of cells in S phase | 25028469 |
| 449 | Growth Inhibition Assay | 3.33 μM | 24 h | decreases the proportion of cells in S phase | 25028469 |
| 778 | Growth Inhibition Assay | 3.33 μM | 24 h | decreases the proportion of cells in S phase | 25028469 |
| LPS141 | Growth Inhibition Assay | 3.33 μM | 24 h | decreases the proportion of cells in S phase | 25028469 |
| KOPN8 | Apoptosis assay | 0.5 uM | 3 hrs | Induction of apoptosis in human KOPN8 cells assessed as upregulation of cleaved PARP level at 0.5 uM after 3 hrs by Western blot analysis | 29407975 |
| KOPN8 | Apoptosis assay | 0.5 uM | 24 hrs | Induction of apoptosis in human KOPN8 cells assessed as upregulation of cleaved PARP level at 0.5 uM pre-treated with NAC for 1 hr and measured after 24 hrs by Western blot analysis | 29407975 |
| Fluc-labeled 4T1 | Antitumor assay | 130 mg/kg | 18 days | Antitumor activity against mouse Fluc-labeled 4T1 cells implanted in Balb/c mouse assessed as reduction in tumor weight at 130 mg/kg, ip administered daily for 18 days measured after 8 to 25 days | 29518312 |
| LPS141 | Growth Inhibition Assay | 72 h | inhibits cell growth dose dependently | 25028469 | |
| LP8 | Growth Inhibition Assay | 72 h | inhibits cell growth dose dependently | 25028469 | |
| LP6 | Growth Inhibition Assay | 72 h | inhibits cell growth dose dependently | 25028469 | |
| LP3 | Growth Inhibition Assay | 72 h | inhibits cell growth dose dependently | 25028469 | |
| 449 | Growth Inhibition Assay | 72 h | inhibits cell growth dose dependently | 25028469 | |
| 778 | Growth Inhibition Assay | 72 h | inhibits cell growth dose dependently | 25028469 | |
| Rh30 | Growth Inhibition Assay | 72 h | IC50＞10000 nM | 25810375 | |
| Rh5 | Growth Inhibition Assay | 72 h | IC50＞10000 nM | 25810375 | |
| CW9019 | Growth Inhibition Assay | 72 h | IC50=9912 nM | 25810375 | |
| Rh41 | Growth Inhibition Assay | 72 h | IC50=7187 nM | 25810375 | |
| Rh28 | Growth Inhibition Assay | 72 h | IC50=845 nM | 25810375 | |
| SKNAS | Growth Inhibition Assay | 72 h | IC50＞10000 nM | 25810375 | |
| IMRS | Growth Inhibition Assay | 72 h | IC50=873 nM | 25810375 | |
| Myoblast | Growth Inhibition Assay | 72 h | IC50=1035 nM | 25810375 | |
| DFSP105 | Growth Inhibition Assay | 24 h | GI50=276 nM | 25852058 | |
| IMR5 | Growth Inhibition Assay | 24 h | IC50=126 nM | 24045179 | |
| BE2C | Growth Inhibition Assay | 24 h | IC50=134 nM | 24045179 | |
| 1643 | Growth Inhibition Assay | 24 h | IC50=147 nM | 24045179 | |
| SKNSH | Growth Inhibition Assay | 24 h | IC50=148 nM | 24045179 | |
| SY5Y | Growth Inhibition Assay | 24 h | IC50=154 nM | 24045179 | |
| NGP | Growth Inhibition Assay | 24 h | IC50=175 nM | 24045179 | |
| KELLY | Growth Inhibition Assay | 24 h | IC50=220 nM | 24045179 | |
| CHP134 | Growth Inhibition Assay | 24 h | IC50=273 nM | 24045179 | |
| NLF | Growth Inhibition Assay | 24 h | IC50=328 nM | 24045179 | |
| LAN5 | Growth Inhibition Assay | 24 h | IC50=429 nM | 24045179 | |
| NB69 | Growth Inhibition Assay | 24 h | IC50=738 nM | 24045179 | |
| SKNDZ | Growth Inhibition Assay | 24 h | IC50=801 nM | 24045179 | |
| NBSD | Growth Inhibition Assay | 24 h | IC50=1900 nM | 24045179 | |
| SKNF1 | Growth Inhibition Assay | 24 h | IC50=3500 nM | 24045179 | |
| EBC1 | Growth Inhibition Assay | 24 h | IC50=6400 nM | 24045179 | |
| SKNAS | Growth Inhibition Assay | 24 h | IC50＞10000 nM | 24045179 | |
| NB16 | Growth Inhibition Assay | 24 h | IC50＞10000 nM | 24045179 | |
| RPE1 | Growth Inhibition Assay | 24 h | IC50＞10000 nM | 24045179 | |
| Sf21 | Function assay | 10 mins | Inhibition of recombinant human full length N-terminal GST-tagged CDK4/Cyclin-D3 co-expressed in baculovirus infected sf21 cells using Rb substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method, IC50 = 0.013 μM. | 29518312 | |
| Sf21 | Function assay | 10 mins | Inhibition of recombinant human full length C-terminal 6His-tagged CDK9/Cyclin-T1 co-expressed in baculovirus infected sf21 cells using PDKtide substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method, IC50 = 0.197 μM. | 29518312 | |
| HepG2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.2862 μM. | 29407975 | |
| SEM | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SEM cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.4605 μM. | 29407975 | |
| KOPN8 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.5008 μM. | 29407975 | |
| NCI-H1299 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 5.46 μM. | 29518312 | |
| T47D | Growth inhibition assay | 72 hrs | Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay, IC50 = 6.227 μM. | 28651979 | |
| T47D | Cytotoxicity assay | 72 hrs | Cytotoxicity against human T47D cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 6.23 μM. | 29518312 | |
| H1299 | Growth inhibition assay | 72 hrs | Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay, IC50 = 7.637 μM. | 28651979 | |
| Hep3B | Cell cycle assay | 24 hrs | Cell cycle arrest in human Hep3B cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry | 29518312 | |
| HepG2 | Cell cycle assay | 24 hrs | Cell cycle arrest in human HepG2 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry | 29518312 | |
| A549 | Cell cycle assay | 24 hrs | Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry | 29518312 | |
| NCI-H460 | Cell cycle assay | 24 hrs | Cell cycle arrest in human NCI-H460 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry | 29518312 | |
| T47D | Cell cycle assay | 24 hrs | Cell cycle arrest in human T47D cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry | 29518312 | |
| MDA-MB-231 | Cell cycle assay | 24 hrs | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry | 29518312 | |
| T47D | Cell cycle assay | 24 hrs | Induction of cell cycle arrest in human T47D cells assessed as increase in G0/G1 phase accumulation incubated for 24 hrs by flow cytometry | 28651979 | |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Ribociclib是一种可口服的，高度特异性CDK4/6抑制剂。 | ||||
|---|---|---|---|---|---|
| 特性 | 口服生物有效的CDK4/6选择性抑制剂，处于Ⅲ期临床测试，用于晚期乳腺癌的治疗。 | ||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | LEE011是一种CDK4/CDK6的双重抑制剂，能够显著抑制17种神经细胞瘤中的12种的生长，平均IC50值是307 nM。对神经细胞瘤的抑制主要是抑制细胞的生长，受到G1细胞周期阻滞和细胞衰老的调控。 |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1细胞系。 | ||
| 浓度 | 10 μM | |||
| 孵育时间 | ~100小时 | |||
| 方法 | 将板中优先附着基底生长的神经母细胞瘤细胞系以一式三份种植于Xcelligence实时细胞电子传感系统，用4个剂量梯度的抑制剂和DMSO为对照处理细胞24小时。连续监测细胞约100个小时，IC50通过以下方法测得：通过绘制细胞指数为时间的函数产生生长曲线，以在治疗开始时细胞指数为1作为标准。从治疗开始到处理96小时后，生长曲线下的面积通过基线下面积为1（治疗开始时的细胞指数）进行计算。积分面积以DMSO处理的对照组作为背景。抑制剂比上对照组的值取非线性对数值来计算。所有的实验至少重复一次。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP |
|
29789630 | |
| Growth inhibition assay | Cell viability |
|
26390342 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | LEE011 (200 mg/kg 每日，口服)引起小鼠中的BE2C 或者 1643细胞显著的生长延迟，没有体重减轻或者其它的毒性症状。[1] |
|
|---|---|---|
| 动物实验 | Animal Models | BE2C, NB-1643,或EBC1异种移植的小鼠。 |
| Dosages | ~200毫克/千克 每天 | |
| Administration | 口服 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05843253 | Not yet recruiting | High Grade Glioma|Diffuse Intrinsic Pontine Glioma|Anaplastic Astrocytoma|Glioblastoma|Glioblastoma Multiforme|Diffuse Midline Glioma H3 K27M-Mutant|Metastatic Brain Tumor|WHO Grade III Glioma|WHO Grade IV Glioma |
Nationwide Children''s Hospital|Novartis |
May 30 2024 | Phase 2 |
| NCT06075758 | Recruiting | Breast Cancer |
Novartis Pharmaceuticals|Novartis |
March 7 2024 | -- |
| NCT05996107 | Recruiting | Breast Cancer |
University of Michigan Rogel Cancer Center |
February 27 2024 | Phase 1 |
化学信息&溶解度
| 分子量 | 434.54 | 分子式 | C23H30N8O |
| CAS号 | 1211441-98-3 | SDF | Download Ribociclib SDF |
| Smiles | CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 8 mg/mL ( (18.41 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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