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

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Quality Control

Batch: Purity: 99.85%

99.85

Related Targets	HDAC JAK Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other BET Inhibitors	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

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 74 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	370.4	Formula	C₂₀H₂₂N₂O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1044870-39-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RVX-000222			Smiles	CC1=CC(=CC(=C1OCCO)C)C2=NC3=C(C(=CC(=C3)OC)OC)C(=O)N2

Mechanism of Action

Features	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), a BET bromodomain inhibitor, preferentially binds to the second bromodomain found on BET proteins. As a stimulator of apolipoprotein (APO) AI gene expression, it increases apoA-I and HDL-C in vitro.
In vivo	Apabetalone (RVX-208) significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24248379/ [2] https://pubmed.ncbi.nlm.nih.gov/20178050/ [3] https://pubmed.ncbi.nlm.nih.gov/20513599/

Applications

Methods	Biomarkers	Images	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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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Handling Instructions

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Apabetalone (RVX-208) BET inhibitor

Chemical Structure

Molecular Weight: 370.4