Apabetalone (RVX-208)

Catalog No.S7295 Synonyms: RVX-000222

For research use only.

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.

Apabetalone (RVX-208) Chemical Structure

CAS No. 1044870-39-4

Selleck's Apabetalone (RVX-208) has been cited by 15 publications

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

Biological Activity

Description 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.
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
BD2 [1]
(Cell-free assay)
0.51 μM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 MYjGeY5kfGmxbjDhd5NigQ>? NVzwfXpnhjZyIN88US=> M{fUdGROW09? M4rib4lv\HWlZYOgZZBwSS2LIH3SUmEh[W6mIHTlJI5wfm9ic4nueIhme2m|IH;mJIFxd0FvST6= NXfPZVU1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVM2QTlpPkKwOVE{PTl7PD;hQi=>
U2OS NELncohHfW6ldHnvckBie3OjeR?= NInwfG5,PSEQvF2= NWPpSZk3\Gm|cHzhZ4V{KEKHVDDwdo91\WmwczDmdo9uKGOqcn;tZZRqdg>? NUf3OVl[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOFg{PzlpPkK0NlQ5Ozd7PD;hQi=>
BL21(DE3)-R3-pRARE2 Mmj3SpVv[3Srb36gZZN{[Xl? MXTJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIFLSSFQh[nKxbX;kc41icW5iMjDlfJBz\XO|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBDVDJzKFTFN{kuWjNvcGLBVmUzKGOnbHzzJJBz\WmwY4XiZZRm\CCob4KgN|AhdWmwczDmc4xtd3enZDDifUBJW0eUR1uoRYMqT0eNKFHjLWdNT0tqQXOpS2dCUyiDYznSTHJMMEKrb4TpckkuV0hicHXweIll\SC|dXLzeJJifGViYXTkbZRqd25iYX\0[ZIhOzBibXnud{BjgSCjbIDoZZMtKEumIE2gNE4yOzVizszNMi=> NUXvNpc4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixPVU4OjNpPkK4NVk2PzJ|PD;hQi=>
BL21(DE3) NELMZWlHfW6ldHnvckBie3OjeR?= M1\6SGJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gRnJFPCCkcn;tc4RwdWGrbjCyJIV5eHKnc4Pl[EBqdiCHc3Po[ZJq[2irYTDjc4xqKEKOMkGgLGRGOyliY3XscJMh[nliaYPveIhmem2jbDD0bZRz[XSrb36gZ4Ftd3KrbXX0dpktKEumIE2gNE4yPCEQvF2u MlrkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|Nke1N|koRjJ4M{[3OVM6RC:jPh?=
BL21(DE3)-R3-pRARE2 NG\4VWRHfW6ldHnvckBie3OjeR?= NGD5TIxKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIFjpd|YufGGpZ3XkJGJTTDNiYoLvcY9ld22jaX6gNkBmgHC{ZYPz[YQhcW5iRYPjbIVzcWOqaXGgZ49tcSCETEKxLGRGOylvUkOtdHJCWkV{IHPlcIx{NCCNZDC9JFAvOTl3IN88UU4> NGTCb5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG5OVczOyd-MkixPVU4OjN:L3G+
BL21(DE3) MnP1SpVv[3Srb36gZZN{[Xl? MVPCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIFLSSFIh[nKxbX;kc41icW5iMjDlfJBz\XO|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBDVDJzIDjESVMqKGOnbHzzJIJ6KGm|b4To[ZJu[WxidHn0doF1cW:wIHPhcI9zcW2ndIL5MEBM\CB;IECuNlUh|ryPLh?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN4N{WzPUc,OjZ|Nke1N|k9N2F-
BL21(DE3)-R3-pRARE2 NEXONm9HfW6ldHnvckBie3OjeR?= MYjJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIFLSSFIh[nKxbX;kc41icW5iMjDlfJBz\XO|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBDVDJzKFTFN{kuWjNvcGLBVmUzKGOnbHzzMEBM\CB;IECuNlUyKM7:TT6= NXrIXnFxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixPVU4OjNpPkK4NVk2PzJ|PD;hQi=>
BL21(DE3) MVHGeY5kfGmxbjDhd5NigQ>? NE[5fm5DcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJGJTTDRiYoLvcY9ld22jaX6gNUBmgHC{ZYPz[YQhcW5iRYPjbIVzcWOqaXGgZ49tcSCETEKxJEhFTTNrIHPlcIx{KGK7IHnzc5Rp\XKvYXygeIl1emG2aX;uJINidG:{aX3leJJ6NCCNZDC9JFEvOSEQvF2u MoTsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|Nke1N|koRjJ4M{[3OVM6RC:jPh?=
BL21(DE3)-R3-pRARE2 Mn;3SpVv[3Srb36gZZN{[Xl? NFzZU|FKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIFjpd|YufGGpZ3XkJGJTTDRiYoLvcY9ld22jaX6gNUBmgHC{ZYPz[YQhcW5iRYPjbIVzcWOqaXGgZ49tcSCETEKxLGRGOylvUkOtdHJCWkV{IHPlcIx{KHC{ZXnuZ5Vj[XSnZDDmc5IhOzBibXnud{Bnd2yub4fl[EBjgSCKNFu1ZYNMQGGlS{GyZYNMOT[jYzDw[ZB1cWSnIIP1ZpN1emG2ZTDh[IRqfGmxbjDh[pRmeiB|MDDtbY5{KGK7IHHsdIhie2O{ZXXuJIF{e2G7LDDL[EA:KDFwMUSyJO69VS5? NULico02RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixPVU4OjNpPkK4NVk2PzJ|PD;hQi=>
SAE NEnldZpHfW6ldHnvckBie3OjeR?= MVOyOEBpenN? MUnJcohq[mm2aX;uJI9nKEKURESgbY4hcHWvYX6gV2FGKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDUUHI{KGGpb37pd5QheG:ueTjJPmMqKC2rbnT1Z4VlKEmVR{W0JHJPSSCneIDy[ZN{cW:wIIDy[Ylv[3WkYYTl[EBnd3JiMkSgbJJ{KG[xbHzve4VlKGK7IIDvcJkpUTqFKTDh[IRqfGmxbjDhcoQhdWWjc4Xy[YQh[W[2ZYKgOEBpenNiYomgV3lDWiCpcnXlckBlgWVvYnHz[YQheVKWLWDDVkBidmGueYPpd{whUUN3MDC9JFIvPjNizszNMi=> M4L1ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkS5O|QyLz5{OU[0PVc1OTxxYU6=
SAE MmPtSpVv[3Srb36gZZN{[Xl? NYfMXHZHOjRiaILz MV\Jcohq[mm2aX;uJI9nKEKURESgbY4hcHWvYX6gV2FGKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDUUHI{KGGpb37pd5QheG:ueTjJPmMqKC2rbnT1Z4VlKEmVR{W2JHJPSSCneIDy[ZN{cW:wIIDy[Ylv[3WkYYTl[EBnd3JiMkSgbJJ{KG[xbHzve4VlKGK7IIDvcJkpUTqFKTDh[IRqfGmxbjDhcoQhdWWjc4Xy[YQh[W[2ZYKgOEBpenNiYomgV3lDWiCpcnXlckBlgWVvYnHz[YQheVKWLWDDVkBidmGueYPpd{whUUN3MDC9JFIvPzRizszNMi=> NIjtfFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[0PVc1OSd-Mkm2OFk4PDF:L3G+
SAE M4\0UmZ2dmO2aX;uJIF{e2G7 NVfYVmp[OjRiaILz NYfERpNEUW6qaXLpeIlwdiCxZjDCVmQ1KGmwIHj1cYFvKFODRTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hXEyUMzDh[49vcXO2IIDvcJkpUTqFKTCtbY5lfWOnZDDndo9j\XSjIGLORUBmgHC{ZYPzbY9vKHC{ZXnuZ5Vj[XSnZDDmc5IhOjRiaILzJIZwdGyxd3XkJIJ6KHCxbImoTVpEMSCjZHTpeIlwdiCjbnSgcYVie3W{ZXSgZYZ1\XJiNDDodpMh[nliU2nCVkBoemWnbjDkfYUu[mG|ZXSgdXJVNVCFUjDhcoFtgXOrczygTWM2OCB;IEOuO|Mh|ryPLh?= MnvEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4NEm3OFEoRjJ7NkS5O|QyRC:jPh?=
SAE MXvGeY5kfGmxbjDhd5NigQ>? Mof6NlQhcHK| MX3Jcohq[mm2aX;uJI9nKEKURESgbY4hcHWvYX6gV2FGKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDUUHI{KGGpb37pd5QheG:ueTjJPmMqKC2rbnT1Z4VlKEmOLUigVm5CKGW6cILld5Nqd25icILlbY5kfWKjdHXkJIZweiB{NDDodpMh\m:ubH;3[YQh[nlicH;sfUhKQkNrIHHk[Il1cW:wIHHu[EBu\WG|dYLl[EBi\nSncjC0JIhzeyCkeTDTXWJTKGe{ZXXuJIR6\S2kYYPl[EByWlRvUFPSJIFv[Wy7c3nzMEBKSzVyIE2gN{45PSEQvF2u NG\6UYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[0PVc1OSd-Mkm2OFk4PDF:L3G+
BL21(DE3)-R3-pRARE2 MYfGeY5kfGmxbjDhd5NigQ>? MVfJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIFLSSFMh[nKxbX;kc41icW5iMTDlfJBz\XO|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBDVDJzKFTFN{kuWjNvcGLBVmUzKGOnbHzzMEBM\CB;IESuNFY2KM7:TT6= NH7mbJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG5OVczOyd-MkixPVU4OjN:L3G+
MV4-11 NWTwZ3F5SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M2TpflczKGi{cx?= MonPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkStNVEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IESuOFgh|ryPLh?= NFnWVIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe2OVAyOyd-Mki3OlUxOTN:L3G+
BL21(DE3)-R3-pRARE2 M1;yR2Z2dmO2aX;uJIF{e2G7 MlfBTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDCVmQzKGK{b33v[I9u[WmwIEGg[ZhxemW|c3XkJIlvKEW|Y3jldolkcGmjIHPvcIkhSkx{MTjESVMqNVJ|LYDSRXJGOiClZXzsd{whU2RiPTC1Mlc5KM7:TT6= NGiyVHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG5OVczOyd-MkixPVU4OjN:L3G+
BL21(DE3) MnXOSpVv[3Srb36gZZN{[Xl? MUfCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIFLSSFIh[nKxbX;kc41icW5iMTDlfJBz\XO|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBDVDJzIDjESVMqKGOnbHzzJIJ6KGm|b4To[ZJu[WxidHn0doF1cW:wIHPhcI9zcW2ndIL5MEBM\CB;IEWuPEDPxE1w M4Gye|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{[3OVM6Lz5{NkO2O|U{QTxxYU6=
OCI-AML3 MlzaRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NV;SbpIyPzJiaILz NFv3XY5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;DTU1CVUx|IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUA4NjF5IN88UU4> NIGyeoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe2OVAyOyd-Mki3OlUxOTN:L3G+
OCI-AML2 NW[xZldqSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MVW3NkBpenN? NUS4OGZySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPR2kuSU2OMjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hQC5|MTFOwG0v NX\Xd|JORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3OlUxOTNpPkK4O|Y2ODF|PD;hQi=>
MCF7 M1LOdWF2fG:yaHHnfUBie3OjeR?= MlrlNVUxKHWP MmXaTY5lfWO2aX;uJI9nKGG3dH;wbIFogSCrbjDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIRwf26{ZXf1cIF1cW:wIH;mJJA3Oi:VUWPUUVEh\XiycnXzd4lwdiCjdDCxOVAhfU1iYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M3TFO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUeyOVQxLz5{OUG3NlU1ODxxYU6=
MDA-MB-231 NXrJR5RDSXW2b4DoZYd6KGG|c3H5 MWCxOVAhfU1? MlzzTY5lfWO2aX;uJI9nKGG3dH;wbIFogSCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG|c3Xzd4VlKGG|IHTve45z\We3bHH0bY9vKG:oIIC2Nk9UWVOWTUGg[ZhxemW|c3nvckBifCBzNUCgeW0h[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz M1;SfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUeyOVQxLz5{OUG3NlU1ODxxYU6=
Assay
Methods Test Index 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 31300040
Immunofluorescence monocyte adhesion ; DNA SARS-CoV-2 CTNT 31300040 33811809
In vivo RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. [3]

Protocol (from reference)

Animal Research:

[3]

  • Animal Models: Naïve adult male AGMs
  • Dosages: ~60 mg/kg
  • Administration: Oral gavage or intravenous administration

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% CMC Na (1N HCl, PH 2.5-3.0)
For best results, use promptly after mixing.

8mg/mL

Chemical Information

Molecular Weight 370.4
Formula

C20H22N2O5

CAS No. 1044870-39-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=CC(=C1OCCO)C)C2=NC3=C(C(=CC(=C3)OC)OC)C(=O)N2

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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
%DMSO %

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03160430 Unknown status Drug: apabetalone|Drug: Placebos Kidney Failure Chronic Resverlogix Corp March 1 2020 Phase 1|Phase 2
NCT03228940 Unknown status Drug: RVX000222 Fabry Disease Resverlogix Corp September 30 2019 Phase 1|Phase 2
NCT01863225 Terminated Drug: RVX000222|Drug: Rosuvastatin|Drug: Atorvastatin Dyslipidemia|Coronary Artery Disease Resverlogix Corp|South Australian Health and Medical Research Institute May 2013 Phase 2
NCT01728467 Completed Drug: RVX000222|Drug: Placebo RVX000222 Diabetes Resverlogix Corp|Baker Heart and Diabetes Institute|Nucleus Network Ltd November 2012 Phase 2
NCT01067820 Completed Drug: RVX000222|Drug: Placebo RVX000222 Coronary Artery Disease Resverlogix Corp|The Cleveland Clinic September 2011 Phase 2
NCT01423188 Completed Drug: RVX000222|Drug: Placebo RVX000222 Coronary Artery Disease|Dyslipidemia Resverlogix Corp|The Cleveland Clinic August 2011 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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