INCB054329

SKU: orb1704822

Description

INCB054329

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1628607-64-6
• MW: 348.36
• Purity: 99.52%
• Formula: C₁₉H₁₆N₄O₃
• SMILES: Cc1noc(C)c1-c1ccc2[nH]c(=O)n3[C@H](COc1c23)c1ccccn1
• Target: Epigenetic Reader Domain
• Solubility: DMSO:100 mg/mL (287.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (11.48 mM)

Bioactivity

• Target IC50:
  BRD4 BD2:3 nM|BRD4 BD1:28 nM|BRD3 BD2:1 nM|BRD3 BD1:9 nM|BRD2 BD2:5 nM
• In Vivo:
  INCB054329 exhibits high clearance in mice leading to a short half-life. At exposures that effectively suppressed c-MYC, INCB054329 is found to be efficacious and well tolerated in both the MM1.S and KMS-12-BM xenograft models. In vivo, oral administration of INCB054329 inhibits tumor growth in several hematologic cancers models.
• 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 GI50 of INCB054329 is 152 nM (range, 26-5000 nM). In contrast to tumor cell lines, the GI50 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. Treatment with INCB054329 inhibits expression of c-MYC and induced HEXIM1 in myeloma cell lines. In both lymphoma and AML cell lines, INCB054329 induces apoptosis consistent with increased expression of pro-apoptotic regulators. INCB054329 reduces expression of Homologous recombination (HR) components and co-operatively reduces cell growth and increases DNA damage and apoptosis induced by cisplatin and PARPi .
• Cell Research:
  Cell lines: DLBCL, AML, Myeloma cells. Incubation Time: 72 h. Method: Cell viability assay
• Animal Research:
  Animal Models: KMS-12-BM tumors established in female Nu/Nu mice. Dosages: 3, 10, 30, or 100 mg/kg. Administration: oral gavage.

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRD4-BD1, BRD4-BD2, BRD3-BD1, BRD3-BD2, BRD2-BD2, EpigeneticReaderDomain, Epigenetic Reader Domain, INCB 054329, INCB54329, INCB-54329, INCB-054329, INCB-054329,INCB 54329, INCB-054329,INCB54329, INCB-054329,INCB-54329, INCB054329, INCB-054329, INCB 54329, inhibit, Inhibitor

Compound Identifiers

PubChem CID

90410660