A BRD2, BRD4, and BRDT inhibitor
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ABBV-075

Item No. 21033

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-(2,4-difluorophenoxy)-3-(6,7-dihydro-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]-ethanesulfonamide
CAS Number
1445993-26-9
Synonyms
  • Mivebresib
Molecular Formula
C22H19F2N3O4S
Formula Weight
459.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: 1 mg/mlDMSO: 20 mg/ml
λmax
229, 297 nm
SMILES
O=S(NC1=CC=C(OC2=CC=C(F)C=C2F)C(C3=CN(C)C(C4=C3C=CN4)=O)=C1)(CC)=O
InChi Code
InChI=1S/C22H19F2N3O4S/c1-3-32(29,30)26-14-5-7-19(31-20-6-4-13(23)10-18(20)24)16(11-14)17-12-27(2)22(28)21-15(17)8-9-25-21/h4-12,25-26H,3H2,1-2H3
InChi Key
RDONXGFGWSSFMY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Cayman Chemical
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    Product Description

    ABBV-075 is a potent inhibitor of the bromodomain and extra terminal domain (BET) family of proteins that is selective for the bromodomain-containing proteins (BRD) BRD2, BRD4, and BRDT (Kis = 1-2.2 nM) over BRD3 (Ki = 12.2 nM) and against a panel of 18 BRD proteins.1 It inhibits BRD4 recruitment to androgen receptor-occupied gene enhancer sites leading to growth inhibition in androgen receptor-dependent prostate cancer cells.2 ABBV-075 halts the cell cycle in the G1 phase and induces apoptosis in prostate cancer cells as well as patient-derived acute myeloid leukemia (AML), non-Hodgkin lymphoma, and multiple myeloma cells.3 It is also efficacious in many xenograft mouse models including lung and prostate cancers, AML, and multiple myeloma.1,2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sarthy, A., Li, L., Albpert, D.H., et al. Abstract 4718: ABBV-075, a novel BET family bromodomain inhibitor, represents a promising therapeutic agent for a broad spectrum of cancer indications. Cancer Res. 76 (14 Suppl), (2016).

    2. Faivre, E.J., Wilcox, D., Lin, X., et al. Exploitation of castration-resistant prostate cancer transcription factor dependencies by the novel BET inhibitor ABBV-075. Mol. Cancer Res. 15(1), 35-44 (2017).

    3. Bui, M.H., Lin, X., Albert, D.H., et al. Preclinical characterization of BET family bromodomain inhibitor ABBV-075 suggests combination therapeutic strategies. Cancer Res. 77(11), 2976-2989 (2017).