Name: Apabetalone (RVX-208)
Brand: Selleck Chemicals
SKU: S7295
Rating: 5 (22 reviews)

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Control de calidad

Lote: Pureza: 99.85%

99.85

Dianas relacionadas	HDAC JAK Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Otros BET Inhibidores	Pelabresib (CPI-0610) ZEN-3694 (BET-IN-19) Molibresib (I-BET-762) Mivebresib (ABBV-075) INCB054329 Birabresib (OTX015) I-BET151 (GSK1210151A) AZD5153 6-hydroxy-2-naphthoic acid CPI-203 I-BRD9

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Formulación	Descripción de la actividad	PMID
HepG2	Function assay	~60 μM		DMSO	induces apoA-I mRNA and de novo synthesis of apoA-I.	20513599
U2OS	Function assay	~5 μM			displaces BET proteins from chromatin	24248379
BL21(DE3)-R3-pRARE2	Function assay				Inhibition of recombinant human His6-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH peptide substrate addition after 30 mins by alphas, Kd = 0.135 μM.	28195723
BL21(DE3)	Function assay				Binding affinity to human BRD4 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry, Kd = 0.14 μM.	26367539
BL21(DE3)-R3-pRARE2	Function assay				Inhibition of recombinant human His6-tagged BRD3 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells, Kd = 0.195 μM.	28195723
BL21(DE3)	Function assay				Binding affinity to human BRD2 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry, Kd = 0.25 μM.	26367539
BL21(DE3)-R3-pRARE2	Function assay				Inhibition of recombinant human His6-tagged BRD2 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells, Kd = 0.251 μM.	28195723
BL21(DE3)	Function assay				Binding affinity to human BRD4 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry, Kd = 1.1 μM.	26367539
BL21(DE3)-R3-pRARE2	Function assay				Inhibition of recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by H4K5acK8acK12acK16ac peptide substrate addition after 30 mins by alphascreen assay, Kd = 1.142 μM.	28195723
SAE	Function assay		24 hrs		Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG54 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis, IC50 = 2.63 μM.	29649741
SAE	Function assay		24 hrs		Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG56 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis, IC50 = 2.74 μM.	29649741
SAE	Function assay		24 hrs		Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced grobeta RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis, IC50 = 3.73 μM.	29649741
SAE	Function assay		24 hrs		Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced IL-8 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis, IC50 = 3.85 μM.	29649741
BL21(DE3)-R3-pRARE2	Function assay				Inhibition of recombinant human His6-tagged BRD3 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells, Kd = 4.065 μM.	28195723
MV4-11	Antiproliferative assay		72 hrs		Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay, IC50 = 4.48 μM.	28765013
BL21(DE3)-R3-pRARE2	Function assay				Inhibition of recombinant human His6-tagged BRD2 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells, Kd = 5.78 μM.	28195723
BL21(DE3)	Function assay				Binding affinity to human BRD2 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry, Kd = 5.8 μM.	26367539
OCI-AML3	Antiproliferative assay		72 hrs		Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay, IC50 = 7.17 μM.	28765013
OCI-AML2	Antiproliferative assay		72 hrs		Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay, IC50 = 8.31 μM.	28765013
MCF7	Autophagy assay	150 uM			Induction of autophagy in human MCF7 cells assessed as downregulation of p62/SQSTM1 expression at 150 uM by Western blot analysis	29172540
MDA-MB-231	Autophagy assay	150 uM			Induction of autophagy in human MDA-MB-231 cells assessed as downregulation of p62/SQSTM1 expression at 150 uM by Western blot analysis	29172540
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Información química, almacenamiento y estabilidad

Peso molecular	370.4	Fórmula	C₂₀H₂₂N₂O₅	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	1044870-39-4	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	RVX-000222			Smiles	CC1=CC(=CC(=C1OCCO)C)C2=NC3=C(C(=CC(=C3)OC)OC)C(=O)N2

Solubilidad

In vitro
Lote:

DMSO : 74 mg/mL (199.78 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.
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

Características	First-in-class BD2-selective inhibitor of BET bromodomain and has been tested in Phase II clinical trials for treatment of coronary syndromes and atherosclerosis.
Targets/IC₅₀/Ki	BD2 (Cell-free assay) 0.51 μM
In vitro	Apabetalone (RVX-208), un inhibidor de BET bromodomain, se une preferentemente al segundo bromodominio que se encuentra en las proteínas BET. Como estimulador de la expresión génica de la apolipoproteína (APO) AI, aumenta apoA-I y HDL-C in vitro.
In vivo	Apabetalone (RVX-208) aumenta significativamente la apoA-I sérica y el HDL-C en AGMs, y mejora el eflujo de colesterol a través de diferentes vías.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/24248379/ [2] https://pubmed.ncbi.nlm.nih.gov/20178050/ [3] https://pubmed.ncbi.nlm.nih.gov/20513599/

Aplicaciones

Métodos	Biomarcadores	Imágenes	PMID
Western blot	p21 / p24 / β-actin cyclin D1 / CDK4 / CDK6 / p24 / β-actin Rb / p-Rb(S780) / p-Rb(S795) / p-Rb(S807/811) / β-actin Cyclin T1 / CDK9-55kDa / CDK9-42kDa / p-CDK9 / CTD / CTD-Ser2P / p24 / β-actin Phospho-RelA / Total-RelA / Actin / BRD2 / α-Tubulin		29789664
Immunofluorescence	monocyte adhesion DNA SARS-CoV-2 CTNT		31300040

Información del ensayo clínico

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

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT03160430	Not yet recruiting	Kidney Failure Chronic	Resverlogix Corp	November 22 2024	Phase 1\|Phase 2
NCT03228940	Withdrawn	Fabry Disease	Resverlogix Corp	November 22 2022	Phase 1\|Phase 2
NCT01863225	Terminated	Dyslipidemia\|Coronary Artery Disease	Resverlogix Corp\|South Australian Health and Medical Research Institute	May 2013	Phase 2
NCT01728467	Completed	Diabetes	Resverlogix Corp\|Baker Heart and Diabetes Institute\|Nucleus Network Ltd	November 2012	Phase 2
NCT01067820	Completed	Coronary Artery Disease	Resverlogix Corp\|The Cleveland Clinic	September 2011	Phase 2
NCT01423188	Completed	Coronary Artery Disease\|Dyslipidemia	Resverlogix Corp\|The Cleveland Clinic	August 2011	Phase 2

Soporte técnico

Instrucciones de manipulación

Tel: +1-832-582-8158 Ext:3

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Apabetalone (RVX-208) BET inhibidor

Estructura química

Peso molecular: 370.4