ARV-825

Catalog No.S8297

For research use only.

ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.

ARV-825 Chemical Structure

CAS No. 1818885-28-7

Selleck's ARV-825 has been cited by 2 Publications

Purity & Quality Control

Choose Selective PROTAC Inhibitors

Biological Activity

Description ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.
Targets
BRD4 BD2 [1]
(Cell-free assay)
BRD4 BD1 [1]
(Cell-free assay)
28 nM(Kd) 90 nM(Kd)
In vitro

Compared with the BRD4 inhibitors, ARV-825 treatment results in a strikingly more pronounced effect on the levels of c-MYC, and downstream cell proliferation and apoptosis induction in BL (Burkitt’s Lymphoma) cell lines[1]. The IC50s of ARV-825 for all tested cell lines and primary AML cells at 72 hours are in the low nanomolar range (2-50 nM). ARV-825 treatment reduces PIM1 levels and phosphorylation of CXCR4 in AML cells while overexpression of PIM1 or Myc reverses the phenomena[3].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
22RV1 NEPhT4ZHfW6ldHnvckBie3OjeR?= MXWyOEBpenN? MmfiTY5lfWO2aX;uJI9nKEOUQl6tcYVlcWG2ZXSgRnJFPCCmZXfyZYRifGmxbjDpckBpfW2jbjCyNnJXOSClZXzsd{Bu\WG|dYLl[EBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXNuIFTDOVAhRSByLkCwNFU4KM7:TT6= MlT2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4OES4O|EoRjNyNki0PFcyRC:jPh?=
NAMALWA M3LHXWZ2dmO2aX;uJIF{e2G7 NUPBW4oxd3[ncn7p[4h1 NXnQNpI{WHKxdHHjJIFkfGm4aYT5JIF1KEOncnXicI9vN0KURESgbY4hcHWvYX6gUmFOSUyZQTDj[YxteyCjc4Pld5Nm\CCjczDpcoR2[3Srb36gc4YhSlKGNDDwdo91\WmwIHTl[5Ji\GG2aX;uJIlvKGi3bXHuJG5CVUGOV1GgZ4VtdHNiYX\0[ZIhd3[ncn7p[4h1KGmwY4XiZZRqd25iYomgbY1ufW6xYnzveEBu\XSqb3SsJGREPTBiPTCwMlAxOSEQvF2u MoDrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzFyNEe3OFgoRjNzMES3O|Q5RC:jPh?=
CA46 M1rDT2Z2dmO2aX;uJIF{e2G7 NWPOTHlZd3[ncn7p[4h1 MknvVJJwfGGlIHHjeIl3cXS7IHH0JGNmemWkbH;uM2JTTDRiaX6gbJVu[W5iQ1G0OkBk\WyuczDhd5Nme3OnZDDhd{BqdmS3Y4Tpc44hd2ZiQmLEOEBxem:2ZXnuJIRm\3KjZHH0bY9vKGmwIHj1cYFvKEODNE[gZ4VtdHNiYX\0[ZIhd3[ncn7p[4h1KGmwY4XiZZRqd25iYomgbY1ufW6xYnzveEBidmGueYPpd{whTEN3MDC9JFAvODBzIN88UU4> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTB2N{e0PEc,OzFyNEe3OFg9N2F-
MV4-11 MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlvJPVYhcHK| NXO1RZc4T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVVZ2LUGxJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR|UxKD1iMD6wNFExPSEQvF2u MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODBzOUmwNUc,OzByMUm5NFE9N2F-
RS4:11 NVfxSphDS3m2b4TvfIlkcXS7IHHzd4F6 NX7PbGM2PCCmYYnz M2e5eGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJUPDpzMTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQh\GG7czDifUBYW1RvODDhd5NigSxiSVO1NEA:KDBwMECzN{DPxE1w M3mxRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{O5NVk3Lz5{OEOzPVE6PjxxYU6=
RS4:11 MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWO5OkBpenN? NV32bZRFT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2OkGxJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR|UxKD1iMD6wNFM{KM7:TT6= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODBzOUmwNUc,OzByMUm5NFE9N2F-
MV4-11 M{XhW2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M330[lQ5KGi{cx?= MlvMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkStNVEh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGVEPTBiPTCwMlAyPjl6IN88UU4> NHywTI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEW5OVAxPyd-Mki1PVUxODd:L3G+
MOLM13 NHnKcXlEgXSxdH;4bYNqfHliYYPzZZk> M4DYSVQh\GG7cx?= MnW3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUW9NVTF|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgOEBl[Xm|IHL5JHdUXC16IHHzd4F6NCCLQ{WwJF0hOC5yMUiyJO69VS5? NETJ[mU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOzPVE6Pid-MkizN|kyQTZ:L3G+
MOLM13 NIXsUYVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYPKeYp[QTZiaILz NW\KTYNYT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OTUGzJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR|UxKD1iMD6wNVgzKM7:TT6= MoHJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMUm5NFEoRjNyMEG5PVAyRC:jPh?=
HL60 NVi2SG9ESW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Ml\UOFghcHK| NX3WZ4ZiSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBGSzVyIE2gNE4xOzR4NzFOwG0v NV;aSFhbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1PVUxODdpPkK4OVk2ODB5PD;hQi=>
RS4:11 MorTSpVv[3Srb36gZZN{[Xl? MV2zJJRwKDNyIH7N NELJc4s{KGi{cx?= M2C0dGlv\HWldHnvckBw\iClZYLlZoxwdi:ldXzsbY4hPEFvbXXkbYF1\WRiQmLENkBl\We{YXTheIlwdiCrbjDoeY1idiCUU{S6NVEh[2WubIOgZZQhOyC2bzCzNEBvVSCjZoTldkA{KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l M3i1WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{O5NVk3Lz5{OEOzPVE6PjxxYU6=
RS4:11 M4HlVmZ2dmO2aX;uJIF{e2G7 NWP1UZJEOyC2bzCzNEBvVQ>? MofMN{BpenN? NWXjVmFQUW6mdXP0bY9vKG:oIHPldoVjdG:wL3P1cIxqdiB2QT3t[YRq[XSnZDDCVmQ{KGSnZ4Lh[IF1cW:wIHnuJIh2dWGwIGLTOFoyOSClZXzsd{BifCB|IITvJFMxKG6PIHHmeIVzKDNiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? MnTFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|M{mxPVYoRjJ6M{O5NVk3RC:jPh?=
RS4:11 MX3GeY5kfGmxbjDhd5NigQ>? M1n3elMhfG9iM{Cgcm0> NVPQVnllOyCqcoO= M3X2XGlv\HWldHnvckBw\iClZYLlZoxwdi:ldXzsbY4hPEFvbXXkbYF1\WRiQmLEOEBl\We{YXTheIlwdiCrbjDoeY1idiCUU{S6NVEh[2WubIOgZZQhOyC2bzCzNEBvVSCjZoTldkA{KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l NXTSWVBjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizN|kyQTZpPkK4N|M6OTl4PD;hQi=>
U266 MlH5SpVv[3Srb36gZZN{[Xl? NEDPTpYyOiCqcoO= MmW4TY5lfWO2aX;uJI9nKEOUQl6tcYVlcWG2ZXSgRnJFPCCmZXfyZYRifGmxbjDpckBpfW2jbjDVNlY3KGOnbHzzJJVxKHSxIEGwNFAhdk1ibXXhd5Vz\WRiYX\0[ZIhOTJiaILzJIJ6KGmvbYXuc4Jtd3S2aX7nJIFv[Wy7c3nz Mly5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4OES4O|EoRjNyNki0PFcyRC:jPh?=
U266 M1LzfWZ2dmO2aX;uJIF{e2G7 NGK3Z40yOiCqcoO= M{C1SWlv\HWldHnvckBw\iCFUlLOJJVjcXG3aYTpckBtcWejc3WtcYVlcWG2ZXSgTWtbTjFiZHXndoFl[XSrb36gbY4hcHWvYX6gWVI3PiClZXzsd{B2eCC2bzCxNFAxKG6PIH3lZZN2emWmIHHmeIVzKDF{IHjyd{BjgSCrbX31co9jdG:2dHnu[{BidmGueYPpdy=> NEXuOZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|ME[4OFg4OSd-M{C2PFQ5PzF:L3G+
Assay
Methods Test Index PMID
Western blot BRD1 / BRD2 / BRD3 / BRD4 / p21 ; c-MYC ; PARP / cleaved PARP ; CDK6 / CDK4 ; cleaved caspase 9 / cleaved caspase 3 ; Akt / pAKT-S473 / mTOR / p-mTOR-S2448 / p70S6K / p70S6K-T389 / 4EBP1/ p-4EBP1-S65 / PDK1 / p-PDK1-S241 / PI3K / p-PI3K-T458 ; JAK2 / p-STAT5 / p-STAT3 / PIM1 / p27 / Bcl-xl / γH2AX 30903020 26051217 29581547 28042144
Immunofluorescence BRD4 28042144
Growth inhibition assay Cell viability 26051217
In vivo

In a mouse model of human leukemia, the leukemia burdens are significantly lower in the ARV-825 treated mice as confirmed by luciferase imaging, flow cytometry, spleen size and survived longer compared to control mice[3].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: RS4;11 cells
  • Concentrations: 3, 10, 30 nM
  • Incubation Time: 3 h
  • Method:

    RS4;11 cells are treated for 3 h with each individual compound at indicated concentrations, and proteins are probed by specific antibodies.

  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(108.29 mM)
Ethanol 3 mg/mL
(3.24 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 923.43
Formula

C46H47ClN8O9S

CAS No. 1818885-28-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)OCCOCCOCCOCCNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)C8=CC=C(C=C8)Cl)C

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

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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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