Home Epigenetics Epigenetic Reader Domain inhibitor INCB054329 For research use only.

INCB054329

INCB054329 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.

INCB054329 Chemical Structure

INCB054329 Chemical Structure

CAS: 1628607-64-6

Selleck's INCB054329 has been cited by 5 publications

Purity & Quality Control

Batch: Purity: 98.97%
98.97

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Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

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Biological Activity

Description INCB054329 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] Click to View More Targets
1 nM 3 nM 5 nM 9 nM 28 nM
In vitro
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].
Cell Research Cell lines Myeloma, AML, DLBCL cells
Concentrations --
Incubation Time 72 h
Method

Cell viability assay
In Vivo
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].
Animal Research Animal Models KMS-12-BM tumors established in female Nu/Nu mice
Dosages 3, 10, 30, or 100 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02431260 Terminated
Solid Tumors and Hematologic Malignancy
Incyte Corporation
 April 14 2015 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 348.36 Formula

C19H16N4O3
CAS No. 1628607-64-6 SDF --
Smiles CC1=C(C(=NO1)C)C2=C3C4=C(C=C2)NC(=O)N4C(CO3)C5=CC=CC=N5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 70 mg/mL ( (200.94 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 70 mg/mL

Water : ˂1 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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