Mivebresib (ABBV-075)

Catalog No.S8400 Batch:S840002

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Technical Data

Formula

C22H19F2N3O4S
Molecular Weight 459.47 CAS No. 1445993-26-9
Solubility (25°C)* In vitro DMSO 92 mg/mL (200.23 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.
Targets
BRD2 [1] BRD4 [1] BRD-T [1]
In vitro

ABBV-075 exhibits robust single agent activity in cell viability assays across cancer cell lines derived from solid tumors, leukemia and lymphomas. It could disrupt cell cycle control leading to G1 arrest followed by senescence, inhibit oncogenesis drivers leading to apoptosis, and potentially target tumor microenvironment to provide additional therapeutic benefit[1].
In vivo

ABBV-075 has comparable or superior efficacies to standard of care agents in flank xenograft mouse models of non-small-cell and small cell lung cancers, pancreatic, breast, prostate, head & neck cancers, multiple myeloma, diffuse large B cell lymphoma and leukemia[1].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Macrophages

  • Concentrations

    0.1 µM

  • Incubation Time

    48 h

  • Method

    Cells were treated with indicated concentration of drug for 48 h.

Selleck's Mivebresib (ABBV-075) has been cited by 15 publications

Inhibition of bromodomain and extra-terminal proteins targets constitutively active NFκB and STAT signaling in lymphoma and influences the expression of the antiapoptotic proteins BCL2A1 and c-MYC [ Cell Commun Signal, 2024, 22(1):415] PubMed: 39192247
Therapeutic Potential of Bromodomain and Extra-Terminal Domain Inhibitors for Synovial Sarcoma Cells [ Cancers (Basel), 2024, 16(6)1125] PubMed: 38539460
BRD4 plays an antiaging role in the senescence of renal tubular epithelial cells [ Transl Androl Urol, 2024, 13(6):1014-1023] PubMed: 38983468
Pharmacological inhibition of bromodomain and extra-terminal proteins induces an NRF-2-mediated antiviral state that is subverted by SARS-CoV-2 infection [ PLoS Pathog, 2023, 19(9):e1011657] PubMed: 37747932
Targeting the Clear Cell Sarcoma Oncogenic Driver Fusion Gene EWSR1::ATF1 by HDAC Inhibition [ Cancer Res Commun, 2023, 3(7):1152-1165] PubMed: 37405123
Targeting the Clear Cell Sarcoma Oncogenic Driver Fusion Gene EWSR1::ATF1 by HDAC Inhibition [ Cancer Res Commun, 2023, 3(7):1152-1165] PubMed: 37405123
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
Targeting CCR2+ macrophages with BET inhibitor overcomes adaptive resistance to anti-VEGF therapy in ovarian cancer [ J Cancer Res Clin Oncol, 2022, 148(4):803-821] PubMed: 35094142
Targeting CCR2+ macrophages with BET inhibitor overcomes adaptive resistance to anti-VEGF therapy in ovarian cancer [ J Cancer Res Clin Oncol, 2022, 10.1007/s00432-021-03885-z] PubMed: 35094142
Structure-guided discovery of novel potent and efficacious proteolysis targeting chimera (PROTAC) degrader of BRD4 [ Bioorg Chem, 2021, 115:105238] PubMed: 34390970

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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