Apabetalone (RVX-208)

別名：RVX-000222

製品コード：S7295 純度：99.85%

Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.

CAS No. 1044870-39-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
20mg	JPY 40500	国内在庫あり
100mg	JPY 133500	国内在庫あり
1g	JPY 190500	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（18）

カスタマーフィードバック3例

製品安全説明書

現在のバッチを見る：純度： 99.85%

99.85

Apabetalone (RVX-208)関連製品

関連ターゲット	BET p300/CBP BRPF bromodomain	もっと見る
関連製品	ICG-001 Birabresib (OTX015) I-BET151 (GSK1210151A) Molibresib (I-BET-762) SGC-CBP30 EED226 KG-501 CPI-203 compound 3i (666-15) PFI-3 AZD5153 6-hydroxy-2-naphthoic acid PFI-1 (PF-6405761) Mivebresib (ABBV-075) ABBV-744 UNC1215 I-BRD9 Bromosporine PLX51107 GSK1324726A (I-BET726) Pelabresib (CPI-0610) PF-CBP1 HCl INCB054329 MS436 GSK2801 UNC669 MZ-1 NEO2734 OF-1 CPI-637 GSK6853 I-CBP112 BI-7273 PFI-4 INCB057643 GSK 5959 dBET57 BI-9564 Histone Acetyltransferase Inhibitor II	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

シグナル伝達経路

Epigenetic Reader Domainシグナル伝達経路

Epigenetic Reader Domain阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HepG2	Function assay	~60 μM		induces apoA-I mRNA and de novo synthesis of apoA-I.	20513599
U2OS	Function assay	~5 μM		displaces BET proteins from chromatin	24248379
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
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
MV4-11	Antiproliferative assay		72 hrs	Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay, IC50 = 4.48 μM.	28765013
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
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
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
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
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生物活性

製品説明

Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.

特性

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

BD2 ^[1]
(Cell-free assay)

0.51 μM

In Vitro
In vitro	As a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins. ^[1] RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro. ^[2] ^[3]
実験結果図	Methods	Biomarkers	結果図	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

In Vivo
In Vivo	RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. ^[3]
動物実験	動物モデル	Naïve adult male AGMs
	投与量	~60 mg/kg
	投与経路	Oral gavage or intravenous administration

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考
[1] Picaud S, et al. Proc Natl Acad Sci U S A. 2013, 110(49), 19754-19759. [2] McNeill E. Curr Opin Investig Drugs. 2010, 11(3), 357-364. [3] Bailey D, et al. J Am Coll Cardiol. 2010, 55(23), 2580-2589.

参考

化学情報

分子量	370.4	化学式	C₂₀H₂₂N₂O₅
CAS No.	1044870-39-4	SDF	Download Apabetalone (RVX-208) SDFをダウンロードする
Smiles	CC1=CC(=CC(=C1OCCO)C)C2=NC3=C(C(=CC(=C3)OC)OC)C(=O)N2
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个月-20°Cin solvent

In vitro
Batch:

DMSO : 74 mg/mL ( (199.78 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):