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

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.

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BO-264 Chemical Structure

BO-264 Chemical Structure

CAS No. : 2408648-20-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mg USD 150 In-stock
25 mg USD 240 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BO-264 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (141.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.63%

COA (246 KB) HNMR (187 KB) LCMS (110 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8298 mL 14.1491 mL 28.2981 mL 70.7454 mL
5 mM 0.5660 mL 2.8298 mL 5.6596 mL 14.1491 mL
10 mM 0.2830 mL 1.4149 mL 2.8298 mL 7.0745 mL
15 mM 0.1887 mL 0.9433 mL 1.8865 mL 4.7164 mL
20 mM 0.1415 mL 0.7075 mL 1.4149 mL 3.5373 mL
25 mM 0.1132 mL 0.5660 mL 1.1319 mL 2.8298 mL
30 mM 0.0943 mL 0.4716 mL 0.9433 mL 2.3582 mL
40 mM 0.0707 mL 0.3537 mL 0.7075 mL 1.7686 mL
50 mM 0.0566 mL 0.2830 mL 0.5660 mL 1.4149 mL
60 mM 0.0472 mL 0.2358 mL 0.4716 mL 1.1791 mL
80 mM 0.0354 mL 0.1769 mL 0.3537 mL 0.8843 mL
100 mM 0.0283 mL 0.1415 mL 0.2830 mL 0.7075 mL
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BO-264 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BO-2642408648-20-2BO264BO 264FGFRApoptosisFibroblast growth factor receptorTACC3antitumoranti-proliferativemitoticDNAdamagespindleabnormalitiescytotoxicityFGFR3-TACC3ERK1/2phosphorylationInhibitorinhibitorinhibit

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