INCB054329

Catalog No.S8753 Synonyms: INCB-054329, INCB-54329

For research use only.

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.

INCB054329 Chemical Structure

CAS No. 1628607-64-6

Selleck's INCB054329 has been cited by 4 Publications

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

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]
()
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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 (from reference)

Cell Research:

[1]

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

    Cell viability assay

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: KMS-12-BM tumors established in female Nu/Nu mice
  • 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)
Water ˂1 mg/mL
Ethanol '70 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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=NO1)C)C2=C3C4=C(C=C2)NC(=O)N4C(CO3)C5=CC=CC=N5

In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02431260 Terminated Drug: INCB054329 Monotherapy Solid Tumors and Hematologic Malignancy Incyte Corporation April 14 2015 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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