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Apabetalone (RVX-208)

別名: RVX-000222 中文名稱：阿帕他隆

Apabetalone (RVX-208, RVX-000222) 是一種有效的BET bromodomain抑制劑，作用于BD2， 無(wú)細(xì)胞試驗(yàn)中IC50為0.510 μM，比作用于BD1選擇性高170倍。Phase 2。

Apabetalone (RVX-208) Chemical Structure

Apabetalone (RVX-208) Chemical Structure

CAS: 1044870-39-4

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 997 現(xiàn)貨
5mg 807.28 現(xiàn)貨
20mg 2216.17 現(xiàn)貨
100mg 7289.1 現(xiàn)貨
1g 10401.3 現(xiàn)貨
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Apabetalone (RVX-208)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Apabetalone (RVX-208, RVX-000222) 是一種有效的BET bromodomain抑制劑，作用于BD2， 無(wú)細(xì)胞試驗(yàn)中IC50為0.510 μM，比作用于BD1選擇性高170倍。Phase 2。
特性 首創(chuàng)新藥BD2選擇性BET溴結(jié)構(gòu)域蛋白抑制劑在II期臨床試驗(yàn)中進(jìn)行測(cè)試，用于冠狀動(dòng)脈綜合癥和動(dòng)脈粥樣硬化的治療。
靶點(diǎn)
BD2 [1]
(Cell-free assay)
0.51 μM
體外研究(In Vitro)
體外研究活性 作為BET溴結(jié)構(gòu)域蛋白抑制劑，RVX-208優(yōu)先與基于BET蛋白質(zhì)的第二溴結(jié)構(gòu)域蛋白結(jié)合。[1] RVX-208，作為載脂蛋白(APO) AI基因表達(dá)的激動(dòng)劑，在體外增加apoA-I 和 HDL-C。[2] [3]
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 RVX-208顯著增加AGMs中血清apoA-I和 HDL-C，并通過不同途徑增加膽固醇流出。[3]
動(dòng)物實(shí)驗(yàn) Animal Models 天然成年雄性 AGMs
Dosages ~60 毫克/千克
Administration 口服灌胃或靜脈注射
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

化學(xué)信息&溶解度

分子量 370.4 分子式

C20H22N2O5
CAS號(hào) 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
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 74 mg/mL ( (199.78 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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