BO-264

For research use only.

Catalog No.S8965

BO-264 Chemical Structure

CAS No. 2408648-20-2

BO-264 is a potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with IC50 of 188 nM and Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces SAC-dependent mitotic arrest, apoptosis and DNA damage with antitumor activities.

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Biological Activity

Description BO-264 is a potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with IC50 of 188 nM and Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces SAC-dependent mitotic arrest, apoptosis and DNA damage with antitumor activities.
Targets
FGFR3 [1]
()
TACC3 [1]
(Cell-free assay)
TACC3 [1]
(Cell-free assay)
1.5 nM(Kd) 188 nM
In vitro

BO-264 significantly decreases centrosomal TACC3 during both mitosis and interphase. BO-264 displays potent anti-proliferative activity in the NCI- 60 cell line panel compromising nine different cancer types. BO-264 significantly inhibits the growth of cells harboring FGFR3-TACC3 fusion, an oncogenic driver in diverse malignancies.[1]

In vivo

BO-264's oral administration significantly impairs tumor growth in immunocompromised and immunocompetent breast and colon cancer mouse models, and increases survival without any major toxicity.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: JIMT-1 cells
  • Concentrations: 1 μM
  • Incubation Time: 6 h
  • Method:

    Briefly, JIMT-1 cells are incubated with vehicle or BO-264 (1 μM) for 6 hours. After treatment, cell pellets are resuspended in Tris-buffered saline (TBS) buffer containing protease and phosphatase inhibitors. The cell suspension is divided into 6 PCR tubes and heated for 5 minutes to 45, 46, 47, 48, 49 and 50 ℃. Subsequently, cells are lysed by three repeated freeze-thaw cycles with liquid nitrogen. Soluble proteins are collected with centrifugation at 20,000 g for 20 minutes at 4 ℃ and analyzed by SDS-PAGE followed by western blot analysis.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: female nude mice with xenografts of HER2-positive JIMT-1 cell line
  • Dosages: 25 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 71 mg/mL (200.91 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 353.38
Formula

C18H19N5O3

CAS No. 2408648-20-2
Storage powder
in solvent
Synonyms N/A
Smiles COC1=CC=C(C=C1)C2=NOC(=C2)NC3=NC(=NC=C3)N4CCOCC4

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID