Ribociclib

別名：LEE011

製品コード：S7440 純度：99.99%

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

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
5mg	JPY 29500	国内在庫あり
25mg	JPY 88500	国内在庫あり
100mg	JPY 149500	国内在庫あり
1g	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（95）

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

関連ターゲット	CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK9 CLK Cdc CDK8 CDK12 CDK13 CDK19 CDK11 CDK/cyclin complexes	もっと見る
関連製品	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 Riviciclib hydrochloride (P276-00) CVT-313 TG003 Kenpaullone R547 Atuveciclib (BAY-1143572) YKL-5-124 LDC4297 Enitociclib (BAY 1251152) PF-06873600 Wogonin SU9516 SEL120 (SEL120-34A) hydrochloride THZ531 Senexin A Samuraciclib (ICEC0942) hydrochloride LY2857785 ON123300 CDK2-IN-73 (CDK2-IN-4) NU2058 BRD6989 HLM006474 AS2863619 CDKI-73 MC180295 ML167 Simurosertib Simurosertib NSC95397 NU6027	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

CDK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
臨床試験 (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
[1] Rader J, et al. Clin Cancer Res. 2013, 19(22), 6173-6182. [2] Antonio Marra, Giuseppe Curigliano. NPJ Breast Cancer. 2019 Aug 29;5:27.

参考

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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

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
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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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):