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 3 Publications

Purity & Quality Control

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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 MmXzSpVv[3Srb36gZZN{[Xl? MY[yOEBpenN? MnfPTY5lfWO2aX;uJI9nKEOUQl6tcYVlcWG2ZXSgRnJFPCCmZXfyZYRifGmxbjDpckBpfW2jbjCyNnJXOSClZXzsd{Bu\WG|dYLl[EBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXNuIFTDOVAhRSByLkCwNFU4KM7:TT6= M{XROlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNki0PFcyLz5|ME[4OFg4OTxxYU6=
NAMALWA M3zrW2Z2dmO2aX;uJIF{e2G7 M3vDNo93\XKwaXfoeC=> MlW0VJJwfGGlIHHjeIl3cXS7IHH0JGNmemWkbH;uM2JTTDRiaX6gbJVu[W5iTlHNRWxYSSClZXzsd{Bie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[gRnJFPCCycn;0[YlvKGSnZ4Lh[IF1cW:wIHnuJIh2dWGwIF7BUWFNX0FiY3XscJMh[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nliaX3teY5w[myxdDDt[ZRpd2RuIFTDOVAhRSByLkCwNUDPxE1w NX\TNWE5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwOFc4PDhpPkOxNFQ4PzR6PD;hQi=>
CA46 NHfZWFNHfW6ldHnvckBie3OjeR?= MVTveoVzdmmpaIS= NHjlR5VRem:2YXOgZYN1cX[rdImgZZQhS2W{ZXLsc44wSlKGNDDpckBpfW2jbjDDRVQ3KGOnbHzzJIF{e2W|c3XkJIF{KGmwZIXjeIlwdiCxZjDCVmQ1KHC{b4TlbY4h\GWpcnHkZZRqd25iaX6gbJVu[W5iQ1G0OkBk\WyuczDh[pRmeiCxdnXycolocHRiaX7jeYJifGmxbjDifUBqdW23bn;icI91KGGwYXz5d4l{NCCGQ{WwJF0hOC5yMEGg{txONg>? MlfYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzFyNEe3OFgoRjNzMES3O|Q5RC:jPh?=
MV4-11 MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHHPPHc6PiCqcoO= MkTGS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUXY1NTFzIHPlcIx{KGGodHXyJFk3KGi{czDifUBES0t6IHHzd4F6NCCLQ{WwJF0hOC5yMEGwOUDPxE1w NXjQ[GY5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNVk6ODFpPkOwNFE6QTBzPD;hQi=>
RS4:11 MmLwR5l1d3SxeHnjbZR6KGG|c3H5 NVv2VlU5PCCmYYnz M1jDO2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJUPDpzMTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQh\GG7czDifUBYW1RvODDhd5NigSxiSVO1NEA:KDBwMECzN{DPxE1w NFf4UHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOzPVE6Pid-MkizN|kyQTZ:L3G+
RS4:11 MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFrQ[G86PiCqcoO= MYnHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDSV|Q7OTFiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUAxNjByM{Og{txONg>? M3KyTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEG5PVAyLz5|MECxPVkxOTxxYU6=
MV4-11 NIDNSGpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MYm0PEBpenN? M4O1NWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0MVEyKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBGSzVyIE2gNE4xOTZ7ODFOwG0v MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV7NUCwO{c,Ojh3OUWwNFc9N2F-
MOLM13 MYDDfZRwfG:6aXPpeJkh[XO|YYm= MlXtOEBl[Xm| NIeyNFlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOV0yPMUOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1KGSjeYOgZpkhX1OWLUigZZN{[XluIFnDOVAhRSByLkCxPFIh|ryPLh?= M4rablxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{O5NVk3Lz5{OEOzPVE6PjxxYU6=
MOLM13 NGX2TnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2W0PFk3KGi{cx?= MX3Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNU2xOOTNiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUAxNjBzOEKg{txONg>? Mm\JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMUm5NFEoRjNyMEG5PVAyRC:jPh?=
HL60 MVzBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NEHVfWk1QCCqcoO= M3SyVmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygSWM2OCB;IECuNFM1PjdizszNMi=> NGXhWnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEW5OVAxPyd-Mki1PVUxODd:L3G+
RS4:11 NIj5cnpHfW6ldHnvckBie3OjeR?= M4LGR|MhfG9iM{Cgcm0> MXSzJIhzew>? NUfrVHZ[UW6mdXP0bY9vKG:oIHPldoVjdG:wL3P1cIxqdiB2QT3t[YRq[XSnZDDCVmQzKGSnZ4Lh[IF1cW:wIHnuJIh2dWGwIGLTOFoyOSClZXzsd{BifCB|IITvJFMxKG6PIHHmeIVzKDNiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? M2D2XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{O5NVk3Lz5{OEOzPVE6PjxxYU6=
RS4:11 Mm\5SpVv[3Srb36gZZN{[Xl? MVezJJRwKDNyIH7N M3H3OVMhcHK| M3PyeWlv\HWldHnvckBw\iClZYLlZoxwdi:ldXzsbY4hPEFvbXXkbYF1\WRiQmLEN{Bl\We{YXTheIlwdiCrbjDoeY1idiCUU{S6NVEh[2WubIOgZZQhOyC2bzCzNEBvVSCjZoTldkA{KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l MkPBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|M{mxPVYoRjJ6M{O5NVk3RC:jPh?=
RS4:11 MWfGeY5kfGmxbjDhd5NigQ>? MXmzJJRwKDNyIH7N NGLqbW4{KGi{cx?= NVSwe20yUW6mdXP0bY9vKG:oIHPldoVjdG:wL3P1cIxqdiB2QT3t[YRq[XSnZDDCVmQ1KGSnZ4Lh[IF1cW:wIHnuJIh2dWGwIGLTOFoyOSClZXzsd{BifCB|IITvJFMxKG6PIHHmeIVzKDNiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? NFTTPI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOzPVE6Pid-MkizN|kyQTZ:L3G+
U266 MlvXSpVv[3Srb36gZZN{[Xl? MWKxNkBpenN? NFzyUVFKdmS3Y4Tpc44hd2ZiQ2LCUk1u\WSrYYTl[EBDWkR2IHTl[5Ji\GG2aX;uJIlvKGi3bXHuJHUzPjZiY3XscJMhfXBidH:gNVAxOCCwTTDt[YF{fXKnZDDh[pRmeiBzMjDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> M1HRXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNki0PFcyLz5|ME[4OFg4OTxxYU6=
U266 NF7sfIxHfW6ldHnvckBie3OjeR?= MUSxNkBpenN? NETS[GlKdmS3Y4Tpc44hd2ZiQ2LCUkB2[mmzdXn0bY4hdGmpYYPlMY1m\GmjdHXkJGlMYkZzIHTl[5Ji\GG2aX;uJIlvKGi3bXHuJHUzPjZiY3XscJMhfXBidH:gNVAxOCCwTTDt[YF{fXKnZDDh[pRmeiBzMjDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> Ml7DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4OES4O|EoRjNyNki0PFcyRC:jPh?=
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.

Solubility (25°C)

In vitro

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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