BO-264

SKU: orb1298888

Description

BO-264 is a potent, orally bioavailable small molecule inhibitor of TACC3, demonstrating high affinity with a Kd of 1.5 nM and an IC50 of 188 nM. It serves as a valuable chemical probe for investigating TACC3 function in cancer biology research, supporting both in vitro and in vivo experimental studies.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 2408648-20-2
• MW: 353.38
• Purity: 99.81%
• Formula: C₁₈H₁₉N₅O₃
• SMILES: COc1ccc(cc1)-c1cc(Nc2ccnc(n2)N2CCOCC2)on1
• Target: FGFR,Apoptosis
• Solubility: DMSO:50 mg/mL (141.49 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.66 mM)

Bioactivity

• Target IC50:
  TACC3:188 nM (IC50)|TACC3:1.5 nM (Kd)
• In Vitro:
  BO-264 demonstrated superior antiproliferative activity to the two currently reported TACC3 inhibitors, especially in aggressive breast cancer subtypes, basal and HER2+, via spindle assembly checkpoint-dependent mitotic arrest, DNA damage, and apoptosis, while the cytotoxicity against normal breast cells was negligible. Furthermore, BO-264 significantly decreased centrosomal TACC3 during both mitosis and interphase. BO-264 displayed potent antiproliferative activity ( 90% have less than 1 μmol/L GI50 value) in the NCI-60 cell line panel compromising of nine different cancer types. Noteworthy, BO-264 significantly inhibited the growth of cells harboring FGFR3-TACC3 fusion, an oncogenic driver in diverse malignancies. Importantly, its oral administration significantly impaired tumor growth in immunocompromised and immunocompetent breast and colon cancer mouse models, and increased survival without any major toxicity. Finally, TACC3 expression has been identified as strong independent prognostic factor in breast cancer and strongly prognostic in several different cancers.

Storage & Handling

• Storage: 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

DNA, damage, cytotoxicity, abnormalities, BO264, BO-264, BO 264, antitumor, anti-proliferative, Apoptosis, mitotic, Inhibitor, inhibit, ERK1/2, Fibroblast growth factor receptor, FGFR, FGFR3-TACC3, phosphorylation, TACC3, spindle

Compound Identifiers

PubChem CID

146018837