Home Cytoskeletal Signaling TACC3 inhibitor - FGFR inhibitor - Apoptosis related activator BO-264 For research use only.

BO-264

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.

BO-264 Chemical Structure

BO-264 Chemical Structure

CAS No. 2408648-20-2

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BO-264 Related Products

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models female nude mice with xenografts of HER2-positive JIMT-1 cell line
Dosages 25 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 353.38 Formula

C18H19N5O3
CAS No. 2408648-20-2 SDF --
Smiles COC1=CC=C(C=C1)C2=NOC(=C2)NC3=NC(=NC=C3)N4CCOCC4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 71 mg/mL ( (200.91 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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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.

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