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| 10mg |
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| Targets |
The mechanism of action of borofalan is based on its role as a boron carrier for BNCT. After administration, borofalan is taken up preferentially by tumor cells, which exhibit increased amino acid transport. When the tumor is subsequently irradiated with thermal or epithermal neutrons, the ¹⁰B atoms incorporated into tumor cells capture neutrons. This nuclear reaction generates high-energy alpha particles and lithium nuclei that cause localized DNA damage and cell death in the boron-containing tumor cells. This targeted therapy spares surrounding normal tissues that have lower boron uptake.
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| ln Vitro |
In vitro, borofalan sensitizes B16/F10 melanoma cells to fast and thermal neutron radiation when used at a concentration of 50 µg/ml. Its uptake by tumor cells can be assessed by measuring intracellular boron concentrations using inductively coupled plasma mass spectrometry (ICP-MS). The compound's ability to be selectively taken up by tumor cells over normal cells is a key feature of its activity. Its radiation-sensitizing properties are evaluated in cell-based neutron irradiation experiments.
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| ln Vivo |
In vivo, borofalan is used in BNCT for the treatment of recurrent or locally advanced head and neck cancer. The compound is administered intravenously, and its distribution is assessed by measuring boron concentrations in blood and tumor tissues. After neutron irradiation, tumor response is evaluated by imaging studies (CT, MRI, PET) and histopathological examination. Clinical studies have demonstrated the efficacy of BNCT with borofalan in treating certain types of cancer.
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| Enzyme Assay |
The in vitro activity of borofalan is assessed using cell-based assays for boron uptake and neutron sensitivity. Tumor cells and normal cells are cultured in appropriate media and treated with varying concentrations of borofalan. Intracellular boron concentrations are measured by ICP-MS. The selective uptake of boron by tumor cells over normal cells is calculated as the tumor-to-normal tissue boron concentration ratio. For neutron sensitivity studies, cells are treated with borofalan and then irradiated with thermal or epithermal neutrons. Cell survival is assessed by clonogenic assays or MTT assays.
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| Cell Assay |
For cellular assays, cancer cell lines (e.g., B16/F10 melanoma cells) and normal cell lines are cultured in appropriate media. Cells are treated with various concentrations of borofalan (typically 1-100 µg/mL) for defined periods (1-24 hours). Intracellular boron concentrations are measured by ICP-MS. Cell viability is assessed using standard assays. For neutron irradiation studies, cells are treated with borofalan and then exposed to neutron radiation. Cell survival is assessed by colony formation assays. The radiation sensitization factor is calculated by comparing survival curves with and without borofalan.
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| Animal Protocol |
In vivo, borofalan is typically administered intravenously to patients or animal models. In clinical BNCT, the compound is infused over 1-2 hours, followed by neutron irradiation. Boron concentrations in blood and tumor tissues are monitored throughout the procedure. Tumor response is evaluated by imaging studies and histopathological examination. In animal models, the compound is administered at various doses, and the biodistribution of boron is assessed by measuring boron concentrations in various tissues. Efficacy is assessed by measuring tumor growth inhibition or survival.
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| ADME/Pharmacokinetics |
Borofalan has a molecular weight of 208.21 g/mol and a molecular formula of C9H12¹⁰BNO4. It is a white to off-white powder that is soluble in water and DMSO. The compound should be stored at -20°C under desiccated conditions, protected from light. Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results. The compound's boron-10 content is a critical parameter for its efficacy in BNCT.
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| Toxicity/Toxicokinetics |
Specific toxicity data for borofalan is not available in the provided search results. As a boron carrier for BNCT, its safety profile is primarily related to the distribution of boron in normal tissues and the potential for off-target radiation damage. The compound is intended for use in BNCT under appropriate medical supervision. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies are required to establish its full safety profile.
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| References | |
| Additional Infomation |
Borofalan (10B) is a boronized phenylalanine and boron (boron-10) carrier used in boron neutron capture therapy (BNCT) with potential antitumor activity. After administration, Borofalan (10B) is primarily absorbed by tumor cells. Upon exposure to neutron irradiation, Borofalan (10B) absorbs neutrons and self-destructs, releasing short-range alpha rays and "recoil" lithium into tumor cells, leading to alpha-ray-induced tumor cell death. This highly selective localized radiotargeting therapy protects adjacent normal tissues.
Borofalan is a research compound and therapeutic agent used in boron neutron capture therapy (BNCT) for the treatment of cancer. BNCT is a targeted radiotherapy that selectively destroys tumor cells that have taken up boron-10. Borofalan has been investigated in clinical studies for the treatment of recurrent or locally advanced head and neck cancer. It is not widely approved but is available for research and clinical use in some regions. Its development represents a significant advance in targeted cancer therapy. |
| Molecular Formula |
C9H12BNO4
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|---|---|
| Molecular Weight |
209.0
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| Exact Mass |
208.089
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| CAS # |
80994-59-8
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| Related CAS # |
L-p-Boronophenylalanine;76410-58-7
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| PubChem CID |
25033700
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.591
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
15
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| Complexity |
216
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[10B](C1=CC=C(C=C1)C[C@@H](C(=O)O)N)(O)O
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| InChi Key |
NFIVJOSXJDORSP-ULMHTEDTSA-N
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| InChi Code |
InChI=1S/C9H12BNO4/c11-8(9(12)13)5-6-1-3-7(4-2-6)10(14)15/h1-4,8,14-15H,5,11H2,(H,12,13)/t8-/m0/s1/i10-1
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| Chemical Name |
(2S)-2-amino-3-(4-(10B)dihydroxy(10B)phenyl)propanoic acid
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| Synonyms |
Related CAS# 80994-59-8; L-4-Boronophenylalanine; Borofalan
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~4 mg/mL (~19.21 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7847 mL | 23.9234 mL | 47.8469 mL | |
| 5 mM | 0.9569 mL | 4.7847 mL | 9.5694 mL | |
| 10 mM | 0.4785 mL | 2.3923 mL | 4.7847 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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