A BRD4 inhibitor that drives BRD4 degradation
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ARV-825

Item No. 21109

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)ethoxy)phenyl)acetamide
CAS Number
1818885-28-7
Molecular Formula
C46H47ClN8O9S
Formula Weight
923.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 1 mg/ml
λmax
247, 409 nm
SMILES
CC1=NN=C2[C@H](CC(NC3=CC=C(OCCOCCOCCOCCNC4=C(C(N(C5C(NC(CC5)=O)=O)C6=O)=O)C6=CC=C4)C=C3)=O)N=C(C7=CC=C(Cl)C=C7)C8=C(SC(C)=C8C)N21
InChi Code
InChI=1S/C46H47ClN8O9S/c1-26-27(2)65-46-39(26)41(29-7-9-30(47)10-8-29)50-35(42-53-52-28(3)54(42)46)25-38(57)49-31-11-13-32(14-12-31)64-24-23-63-22-21-62-20-19-61-18-17-48-34-6-4-5-33-40(34)45(60)55(44(33)59)36-15-16-37(56)51-43(36)58/h4-14,35-36,48H,15-25H2,1-3H3,(H,49,57)(H,51,56,58)/t35-,36?/m0/s1
InChi Key
RWLOGRLTDKDANT-TYIYNAFKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 µg

    $54

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    1 mg

    $102

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    5 mg

    $444

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    Cayman Chemical
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    Product Description

    ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.1 ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at < 1 nM).1 In Burkitt’s lymphoma cells, ARV-825 reduces c-Myc levels, blocks cell proliferation, and induces apoptosis.1 The degradation of BRD4 in cells treated with ARV-825 can be blocked with lenalidomide (Item No. 14643), a competitor for binding to cereblon.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lu, J., Qian, Y., Altieri, M., et al. Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4. Chem. Biol. 22(6), 755-763 (2015).

    2. Abruzzese, M.P., Bilotta, M.T., Fionda, C., et al. Inhibition of bromodomain and extra-terminal (BET) proteins increases NKG2D ligand MICA expression and sensitivity to NK cell-mediated cytotoxicity in multiple myeloma cells: role of cMYC-IRF4-miR-125b interplay. J. Hematol. Oncol. 9(1), 134 (2016).