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

Ribociclib Chemical Structure

CAS: 1211441-98-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 794.43 现货
5mg RMB 647.01 现货
25mg RMB 1941.03 现货
100mg RMB 4668.3 现货
1g RMB 7944.3 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

免费分装
免费预溶

客户使用Selleck的Ribociclib发表文献84

产品质控

批次: 纯度: 99.99%
99.98

Ribociclib相关产品

相关信号通路图

CDK抑制剂选择性比较

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
CDK4 [2]
(Cell-free assay)
CDK6 [2]
(Cell-free assay)
10 nM 39 nM
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。

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。

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
NCT06075758 Not yet recruiting
Breast Cancer
Novartis Pharmaceuticals|Novartis
February 9 2024 --
NCT05996107 Recruiting
Breast Cancer
University of Michigan Rogel Cancer Center
January 2024 Phase 1
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
January 15 2024 Phase 2

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)

体外溶解度
批次:

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
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

* 必填项

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们
Tags: buy Ribociclib | Ribociclib supplier | purchase Ribociclib | Ribociclib cost | Ribociclib manufacturer | order Ribociclib | Ribociclib distributor
在线咨询
联系我们