INCB054329(INCB-054329,INCB-54329)

Catalog No.S8753

INCB054329(INCB-054329,INCB-54329) Chemical Structure

Molecular Weight(MW): 348.36

INCB054329(INCB-054329; INCB-54329) is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively.

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Biological Activity

Description INCB054329(INCB-054329; INCB-54329) is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively.
Targets
BRD3-BD2 [1]
()
BRD4-BD2 [1]
()
BRD2-BD2 [1]
()
BRD3-BD1 [1]
()
BRD4-BD1 [1]
()
1 nM 3 nM 5 nM 9 nM 28 nM
In vitro

INCB054329 shows no significant inhibitory activity against 16 non-BET bromodomains at 3 μM. In a panel of 32 hematologic cancer cell lines derived from acute myeloid leukemia, non-Hodgkin lymphoma, and multiple myeloma, the median 50% growth inhibition (GI50) value of INCB054329 is 152 nM (range, 26-5000 nM). In contrast to tumor cell lines, the GI50 value against T cells isolated from non-diseased donors stimulated ex vivo with IL-2 is 2.435 μM. Growth inhibition correlates with a concentration-dependent accumulation of cells in the G1 phase of the cell cycle. INCB054828 is also a selective kinase inhibitor of the FGFR 1, 2, and 3[1]. In myeloma cell lines, treatment with INCB054329 inhibits expression of c-MYC and induced HEXIM1. In both AML and lymphoma cell lines, INCB054329 induces apoptosis consistent with increased expression of pro-apoptotic regulators[2]. INCB054329 reduces expression of Homologous recombination (HR) components and co-operatively reduces cell growth and increases DNA damage and apoptosis induced by PARPi and cisplatin[3].

In vivo

INCB054329 exhibits high clearance in mice resulting in a short half-life. At exposures that effectively suppressed c-MYC, INCB054329 is found to be efficacious and well tolerated in both the KMS-12-BM and MM1.S xenograft models[1]. In vivo, oral administration of INCB054329 inhibits tumor growth in several models of hematologic cancers[2].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: Myeloma, AML, DLBCL cells
  • Concentrations: --
  • Incubation Time: 72 h
  • Method:

    Cell viability assay


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: KMS-12-BM tumors established in female Nu/Nu mice
  • Formulation: first reconstituted in N,N-dimethylacetamide (DMAC), then diluted in a 0.5% methylcellulose solution for a final concentration of 5% DMAC
  • Dosages: 3, 10, 30, or 100 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 70 mg/mL (200.94 mM)
Ethanol 70 mg/mL (200.94 mM)
Water ˂1 mg/mL

* 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 348.36
Formula

C19H16N4O3

CAS No. 1628607-64-6
Storage powder
in solvent
Synonyms N/A

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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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

Tel: +1-832-582-8158 Ext:3

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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID