Apabetalone (RVX-208)

别名: RVX-000222 中文名称：阿帕他隆

目录号：S7295 Purity: 99.85%

Apabetalone (RVX-208, RVX-000222) 是一种有效的BET bromodomain抑制剂，作用于BD2，无细胞试验中IC50为0.510 μM，比作用于BD1选择性高170倍。Phase 2。

Apabetalone (RVX-208) Chemical Structure

CAS: 1044870-39-4

规格	价格	库存
10mM (1mL in DMSO)	RMB 997	现货
5mg	RMB 807.28	现货
20mg	RMB 2216.17	现货
100mg	RMB 7289.1	现货
1g	RMB 10401.3	现货
更大包装有超大折扣
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客户使用Selleck的Apabetalone (RVX-208)发表文献18篇

客户使用该产品的3个实验数据

产品质控

批次：纯度： 99.85%

99.85

Apabetalone (RVX-208)相关产品

相关靶点	BET p300/CBP BRPF bromodomain	点击展开
相关产品	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	点击展开
相关化合物库	激酶抑制剂库 FDA药物库天然产物库已知活性药物库-I 生物活性库Ⅱ	点击展开

Epigenetic Reader Domain抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
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
点击查看更多细胞系数据

生物活性

产品描述

Apabetalone (RVX-208, RVX-000222) 是一种有效的BET bromodomain抑制剂，作用于BD2，无细胞试验中IC50为0.510 μM，比作用于BD1选择性高170倍。Phase 2。

特性

首创新药BD2选择性BET溴结构域蛋白抑制剂在II期临床试验中进行测试，用于冠状动脉综合症和动脉粥样硬化的治疗。

靶点

BD2 ^[1]
(Cell-free assay)

0.51 μM

体外研究(In Vitro)
体外研究活性	作为BET溴结构域蛋白抑制剂，RVX-208优先与基于BET蛋白质的第二溴结构域蛋白结合。^[1] RVX-208，作为载脂蛋白(APO) AI基因表达的激动剂，在体外增加apoA-I 和 HDL-C。^[2] ^[3]
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	Phospho-RelA / Total-RelA / Actin / BRD2 / α-Tubulin Cyclin T1 / CDK9-55kDa / CDK9-42kDa / p-CDK9 / CTD / CTD-Ser2P / p24 / β-actin Rb / p-Rb(S780) / p-Rb(S795) / p-Rb(S807/811) / β-actin cyclin D1 / CDK4 / CDK6 / p24 / β-actin p21 / p24 / β-actin		31300040
	Immunofluorescence	DNA SARS-CoV-2 CTNT monocyte adhesion		33811809

体内研究(In Vivo)
体内研究活性	RVX-208显著增加AGMs中血清apoA-I和 HDL-C，并通过不同途径增加胆固醇流出。^[3]
动物实验	Animal Models	天然成年雄性 AGMs
	Dosages	~60 毫克/千克
	Administration	口服灌胃或静脉注射

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

参考文献
[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.

参考文献

化学信息&溶解度

分子量	370.4	分子式	C₂₀H₂₂N₂O₅
CAS号	1044870-39-4	SDF	Download Apabetalone (RVX-208) SDF
Smiles	CC1=CC(=CC(=C1OCCO)C)C2=NC3=C(C(=CC(=C3)OC)OC)C(=O)N2
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 74 mg/mL ( (199.78 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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