Ribociclib

别名: LEE011 中文名称：瑞博西利，瑞博西林

目录号：S7440 Purity: 99.99%

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

规格	价格	库存
10mM (1mL in DMSO)	794.43	现货
5mg	647.01	现货
25mg	1941.03	现货
100mg	4668.3	现货
1g	7944.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

产品质控

批次：纯度： 99.99%

99.99

Ribociclib相关产品

相关靶点	CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK9 CLK Cdc CDK8 CDK12 CDK13 CDK19 CDK11 CDK/cyclin complexes	点击展开
相关产品	Ro-3306 Dinaciclib Roscovitine Flavopiridol (Alvocidib) SNS-032 (BMS-387032) Flavopiridol (Alvocidib) HCl AT7519 LDC000067 PHA-767491 HCl THZ1 2HCl XL413 JNJ-7706621 AZD5438 Purvalanol A Milciclib BS-181 HCl K03861 (AUZ454) PHA-793887 BMS-265246 AT7519 HCl AZD4573 MSC2530818 R547 Riviciclib hydrochloride (P276-00) (E/Z)-TG003 Kenpaullone CVT-313 Atuveciclib (BAY-1143572) YKL-5-124 LDC4297 Enitociclib (BAY 1251152) SU9516 Wogonin SEL120 (SEL120-34A) hydrochloride THZ531 PF-06873600 ON123300 LY2857785 Senexin A Samuraciclib (ICEC0942) hydrochloride NU6027 ML167 NU2058 MC180295 NSC95397 CDK2-IN-73 (CDK2-IN-4) BRD6989 HLM006474 AS2863619 Simurosertib CDKI-73	点击展开
相关化合物库	激酶抑制剂库 PI3K/Akt 抑制剂库 MAPK抑制剂库 DNA损伤/ DNA修复化合物库细胞周期化合物库	点击展开

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(PMID)
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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
https://pubmed.ncbi.nlm.nih.gov/24045179/ https://pubmed.ncbi.nlm.nih.gov/31482107/

参考文献

https://pubmed.ncbi.nlm.nih.gov/24045179/
https://pubmed.ncbi.nlm.nih.gov/31482107/

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

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

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

DMSO : 22 mg/mL ( (50.62 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 20 mg/mL ( (46.02 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

体内溶解配方批次：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
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	1.100mg/ml (2.53mM)	以 1 mL 工作液为例，取50μL22mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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。

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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Ribociclib

产品质控

Ribociclib相关产品

相关信号通路图

细胞实验数据示例

生物活性

化学信息&溶解度

实验计算

技术支持