Ribociclib

別名:LEE011

Ribociclib is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.

Ribociclib化学構造

CAS No. 1211441-98-3

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 44500 国内在庫あり
JPY 29500 国内在庫あり
JPY 44500 国内在庫あり
JPY 88500 国内在庫あり
JPY 149500 国内在庫あり
JPY 295500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(84)

製品安全説明書

現在のバッチを見る: 純度: 99.99%
99.99

Ribociclib関連製品

シグナル伝達経路

CDK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 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
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生物活性

製品説明 Ribociclib is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.
特性 Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.
Targets
CDK4 [2]
(Cell-free assay)
CDK6 [2]
(Cell-free assay)
10 nM 39 nM
In Vitro
In vitro

LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is mediated by a G1 cell-cycle arrest and cellular senescence. [1]

細胞実験 細胞株 BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1 cell lines.
濃度 10 μM
反応時間 ~100 hours
実験の流れ

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.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP 29789630
Growth inhibition assay Cell viability 26390342
In Vivo
In Vivo

LEE011 (200 mg/kg daily, p.o.) significantly causes tumor growth delay in mice harboring the BE2C or 1643 xenografts with no weight loss or other signs of toxicity. [1]

動物実験 動物モデル Mice bearing BE2C, NB-1643, or EBC1 xenografts.
投与量 ~200 mg/kg daily
投与経路 p.o.
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

化学情報

分子量 434.54 化学式

C23H30N8O

CAS No. 1211441-98-3 SDF Download Ribociclib SDFをダウンロードする
Smiles CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5
保管

In vitro
Batch:

DMSO : 8 mg/mL ( (18.41 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Tags: Ribociclibを買う | Ribociclib ic50 | Ribociclib供給者 | Ribociclibを購入する | Ribociclib費用 | Ribociclib生産者 | オーダーRibociclib | Ribociclib化学構造 | Ribociclib分子量 | Ribociclib代理店