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Ribociclib

別名: LEE011 中文名稱：瑞博西利，瑞博西林

Ribociclib是一種可口服的，高度特異性CDK4/6抑制劑。

Ribociclib Chemical Structure

Ribociclib Chemical Structure

CAS: 1211441-98-3

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 794.43 現(xiàn)貨
5mg 647.01 現(xiàn)貨
25mg 1941.03 現(xiàn)貨
100mg 4668.3 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Ribociclib相關(guān)產(chǎn)品

相關(guān)信號通路圖

CDK Signaling Pathways

CDK信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產(chǎn)品描述 Ribociclib是一種可口服的，高度特異性CDK4/6抑制劑。
特性 口服生物有效的CDK4/6選擇性抑制劑，處于Ⅲ期臨床測試，用于晚期乳腺癌的治療。
靶點
CDK4 [2]
(Cell-free assay)		 CDK6 [2]
(Cell-free assay)
10 nM 39 nM
體外研究(In Vitro)
體外研究活性

LEE011是一種CDK4/CDK6的雙重抑制劑，能夠顯著抑制17種神經(jīng)細胞瘤中的12種的生長，平均IC50值是307 nM。對神經(jīng)細胞瘤的抑制主要是抑制細胞的生長，受到G1細胞周期阻滯和細胞衰老的調(diào)控。
細胞實驗 細胞系 BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1細胞系。
濃度 10 μM
孵育時間 ~100小時
方法

將板中優(yōu)先附著基底生長的神經(jīng)母細胞瘤細胞系以一式三份種植于Xcelligence實時細胞電子傳感系統(tǒng)，用4個劑量梯度的抑制劑和DMSO為對照處理細胞24小時。連續(xù)監(jiān)測細胞約100個小時，IC50通過以下方法測得：通過繪制細胞指數(shù)為時間的函數(shù)產(chǎn)生生長曲線，以在治療開始時細胞指數(shù)為1作為標(biāo)準(zhǔn)。從治療開始到處理96小時后，生長曲線下的面積通過基線下面積為1（治療開始時的細胞指數(shù)）進行計算。積分面積以DMSO處理的對照組作為背景。抑制劑比上對照組的值取非線性對數(shù)值來計算。所有的實驗至少重復(fù)一次。
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
Western blot

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