Name: LEE011 (Ribociclib)
Brand: Selleck Chemicals
SKU: S7440
Rating: 5 (113 reviews)

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Control de calidad (Quality Control)

Lote: Pureza: 99.99%

99.99

Dianas relacionadas	HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase Casein Kinase
Otros CDK Inhibidores	AS2863619 Ro-3306 SEL120 (SEL120-34A) hydrochloride INX-315 Tagtociclib (PF-07104091) PF-07220060 (CDK4/6-IN-6) AZD4573 ON123300 Enitociclib (BAY 1251152) Samuraciclib (ICEC0942) hydrochloride

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Formulación	Descripción de la actividad	PMID
DFSP105	Growth Inhibition Assay		24 h		GI50=276 nM	25852058
Myoblast	Growth Inhibition Assay		72 h		IC50=1035 nM	25810375
IMRS	Growth Inhibition Assay		72 h		IC50=873 nM	25810375
SKNAS	Growth Inhibition Assay		72 h		IC50＞10000 nM	25810375
Rh28	Growth Inhibition Assay		72 h		IC50=845 nM	25810375
Rh41	Growth Inhibition Assay		72 h		IC50=7187 nM	25810375
CW9019	Growth Inhibition Assay		72 h		IC50=9912 nM	25810375
Rh5	Growth Inhibition Assay		72 h		IC50＞10000 nM	25810375
Rh30	Growth Inhibition Assay		72 h		IC50＞10000 nM	25810375
778	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
449	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
LP3	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
LP6	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
LP8	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
LPS141	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
778	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
LP3	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
LP8	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
IMR5	Growth Inhibition Assay		24 h	DMSO	IC50=126 nM	24045179
BE2C	Growth Inhibition Assay		24 h	DMSO	IC50=134 nM	24045179
1643	Growth Inhibition Assay		24 h	DMSO	IC50=147 nM	24045179
SKNSH	Growth Inhibition Assay		24 h	DMSO	IC50=148 nM	24045179
SY5Y	Growth Inhibition Assay		24 h	DMSO	IC50=154 nM	24045179
NGP	Growth Inhibition Assay		24 h	DMSO	IC50=175 nM	24045179
KELLY	Growth Inhibition Assay		24 h	DMSO	IC50=220 nM	24045179
CHP134	Growth Inhibition Assay		24 h	DMSO	IC50=273 nM	24045179
NLF	Growth Inhibition Assay		24 h	DMSO	IC50=328 nM	24045179
LAN5	Growth Inhibition Assay		24 h	DMSO	IC50=429 nM	24045179
NB69	Growth Inhibition Assay		24 h	DMSO	IC50=738 nM	24045179
SKNDZ	Growth Inhibition Assay		24 h	DMSO	IC50=801 nM	24045179
NBSD	Growth Inhibition Assay		24 h	DMSO	IC50=1900 nM	24045179
SKNF1	Growth Inhibition Assay		24 h	DMSO	IC50=3500 nM	24045179
EBC1	Growth Inhibition Assay		24 h	DMSO	IC50=6400 nM	24045179
SKNAS	Growth Inhibition Assay		24 h	DMSO	IC50＞10000 nM	24045179
NB16	Growth Inhibition Assay		24 h	DMSO	IC50＞10000 nM	24045179
RPE1	Growth Inhibition Assay		24 h	DMSO	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
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
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
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
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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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	434.54	Fórmula	C₂₃H₃₀N₈O	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	1211441-98-3	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	LEE011			Smiles	CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 8 mg/mL (18.41 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	1.100mg/ml (2.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Características	Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.
Targets/IC₅₀/Ki	CDK4 (Cell-free assay) 10 nM CDK6 (Cell-free assay) 39 nM
In vitro	LEE011, como inhibidor dual de CDK4/CDK6, inhibe significativamente el crecimiento de 12 de 17 líneas celulares de neuroblastoma con una IC50 media de 307 nM. La inhibición del crecimiento de las líneas celulares de neuroblastoma es principalmente citostática y está mediada por una detención del Cell Cycle en G1 y la senescencia celular.
In vivo	LEE011 (200 mg/kg diarios, p.o.) causa un retraso significativo en el crecimiento tumoral en ratones portadores de xenoinjertos BE2C o 1643 sin pérdida de peso u otros signos de toxicidad.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/24045179/ [2] https://pubmed.ncbi.nlm.nih.gov/31482107/

Aplicaciones (Applications)

Métodos	Biomarcadores	Imágenes	PMID
Western blot	pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP		29789630
Growth inhibition assay	Cell viability		26390342

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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

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):

LEE011 (Ribociclib) CDK4/6 inhibitor

Estructura química

Peso molecular: 434.54

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Aplicaciones (Applications)

Información del ensayo clínico (Clinical Trial Information)

LEE011 (Ribociclib) CDK4/6 inhibitor

Estructura química

Peso molecular: 434.54

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo (Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Aplicaciones (Applications)

Información del ensayo clínico (Clinical Trial Information)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)