BO-264

Catalog No.S8965 Batch:S896501

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Technical Data

Formula

C18H19N5O3
Molecular Weight 353.38 CAS No. 2408648-20-2
Solubility (25°C)* In vitro DMSO 71 mg/mL (200.91 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    female nude mice with xenografts of HER2-positive JIMT-1 cell line

  • Dosages

    25 mg/kg

  • Administration

    Oral gavage

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.