1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. FGFR
    Apoptosis
  3. BO-264

BO-264 

Cat. No.: HY-135960
Handling Instructions

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

For research use only. We do not sell to patients.

BO-264 Chemical Structure

BO-264 Chemical Structure

CAS No. : 2408648-20-2

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Description

BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity[1].

IC50 & Target

IC50: 188 nM (Transforming acidic coiled-coil 3 (TACC3))[1]
Kd: 1.5 nM (TACC3)[1]

In Vitro

BO-264 (500 nM; 48 hours; JIMT-1 cells) treatment induces a prominent increase (from 4.1% to 45.6%) in the fraction of apoptotic cells as assessed by Annexin V/PI staining[1].
BO-264 (500 nM; 24 hours; RT112 cells) treatment decreases ERK1/2 phosphorylation, which is a marker for activated FGFR signaling along with a strong mitotic arrest[1].
BO-264 inhibits cell viability with IC50 values of 190 nM, 160 nM, 120 nM, 130 nM and 360 nM for JIMT-1, HCC1954, MDA-MB-231, MDA-MB-436 and CAL51, respectively. BO-264 specifically targets breast cancer cells while sparing normal cells. BO-264 treatment significantly reduces the average colony number of JIMT-1 cells[1].
BO-264 inhibits the viability of cancer cells with FGFR3-TACC3 fusion with IC50 values of 0.3 μM and 3.66 μM for RT112 and RT4, respectively[1].
BO-264 exhibits a remarkable anti-cancer activity against more than 90% of the NCI267 60 human cancer cell lines representing nine different subpanels with GI50 values less than 1 μM[1].
BO-264 induces mitotic arrest (prominent induces p-Histone H3 (Ser10)), apoptosis (cleaved PARP) and DNA damage, causes aberrant spindle formation and reduces centrosomal localization of TACC3 in JIMT-1 cells[1].

Apoptosis Analysis[1]

Cell Line: JIMT-1 cells
Concentration: 500 nM
Incubation Time: 48 hours
Result: Induced a prominent increase (from 4.1% to 45.6%) in the fraction of apoptotic cells as assessed by Annexin V/PI staining.

Western Blot Analysis[1]

Cell Line: RT112 cells
Concentration: 500 nM
Incubation Time: 24 hours
Result: Decreased ERK1/2 phosphorylation.
In Vivo

BO-264 (25 mg/kg; oral administration; daily; for 3-4 weeks; female nude mice) treatment shows a significant suppression of tumor growth. BO-264 is well tolerated since treatment does not causes a significant body weight loss and organ toxicity[1].

Animal Model: Female nude mice injected with JIMT-1 cells[1]
Dosage: 25 mg/kg
Administration: Oral administration; daily; for 3-4 weeks
Result: Showed a significant suppression of tumor growth.
Molecular Weight

353.38

Formula

C₁₈H₁₉N₅O₃

CAS No.

2408648-20-2

SMILES

COC1=CC=C(C2=NOC(NC3=NC(N4CCOCC4)=NC=C3)=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (707.45 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8298 mL 14.1491 mL 28.2981 mL
5 mM 0.5660 mL 2.8298 mL 5.6596 mL
10 mM 0.2830 mL 1.4149 mL 2.8298 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

BO-264BO264BO 264FGFRApoptosisFibroblast growth factor receptorTACC3antitumoranti-proliferativemitoticDNAdamagespindleabnormalitiescytotoxicityFGFR3-TACC3ERK1/2phosphorylationInhibitorinhibitorinhibit

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