| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
BNC-105 targets tubulin, binding to the colchicine binding site. By binding to tubulin, it inhibits tubulin polymerization, blocking the formation of the mitotic spindle. This leads to cell cycle arrest and disruption of tumor angiogenesis. Unlike broad-spectrum antimitotics, BNC-105 is engineered to selectively disrupt the neoangiogenic vasculature that nourishes solid tumors. The compound shows sub-nanomolar potency against proliferating endothelial cells (EC50 = 0.31 nM).
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| ln Vitro |
In vitro, BNC-105 demonstrates potent antiproliferative activity against a panel of cancer cell lines with IC50 <1 nM for DU145, Calu-6, and MDA-MB-231. It inhibits tubulin polymerization by binding to the colchicine site on tubulin. The compound shows sub-nanomolar potency against proliferating endothelial cells (EC50 = 0.31 nM). These properties make BNC-105 a potent vascular disrupting agent for cancer research.
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| ln Vivo |
In vivo, BNC-105 functions as a vascular disrupting agent, selectively disrupting the tumor vasculature. Upon administration, it binds to tubulin and inhibits polymerization, leading to mitotic spindle disruption, cell cycle arrest, and disruption of tumor angiogenesis. The compound has potential anti-angiogenic and antitumor activities. Specific animal model data and dosing regimens are available in the primary literature.
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| Enzyme Assay |
Not specifically documented for BNC-105. For tubulin polymerization inhibitors, cell-free assays typically measure the inhibition of tubulin polymerization using purified tubulin and spectrophotometric detection of polymerization. Competition binding assays using radiolabeled colchicine can confirm binding to the colchicine site on tubulin. These assays determine the mechanism of action and potency of the compound.
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| Cell Assay |
In vitro cell-based assays for BNC-105 include cell proliferation assays in various cancer cell lines (DU145, Calu-6, MDA-MB-231). Endothelial cell proliferation assays assess the compound's effects on angiogenesis. Cell cycle analysis by flow cytometry can evaluate mitotic arrest. The compound shows potent activity with IC50 values in the sub-nanomolar to low nanomolar range.
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| Animal Protocol |
In vivo studies with BNC-105 are conducted in mouse xenograft models of cancer. The compound is administered via various routes depending on the experimental design. Endpoints include tumor growth inhibition, assessment of tumor vascular disruption, and evaluation of antitumor activity. Dosing regimens and specific animal models are detailed in the primary literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for BNC-105 are not extensively documented in the available literature. The compound is a small molecule with molecular weight 372.37. Detailed PK parameters such as half-life, bioavailability, and clearance are available in the primary literature but are not detailed in the available sources.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BNC-105 are not provided in the available literature. As a research compound, it is not intended for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound. The compound is supplied for research purposes only.
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| References |
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| Additional Infomation |
BNC105, a vascular disruptor (VDA), possesses potential anti-angiogenic and antitumor activities. Upon administration, BNC105 binds to tubulin and inhibits its polymerization, thereby blocking the formation of the mitotic spindle, leading to cell cycle arrest and tumor angiogenesis disruption. This deprives tumor cells of nutrients, ultimately resulting in tumor cell apoptosis. In addition to its vascular disruptor activity, this drug also exerts direct cytotoxic effects on tumor cells by inhibiting tubulin polymerization.
See also: BNC-105p free acid (note moved to). BNC-105 is also known as BNC105. It is a benzofuran-derived tubulin polymerization inhibitor and vascular disrupting agent. The compound has potent antiproliferative and tumor vascular disrupting properties. It is used in cancer research to study vascular disruption and tubulin inhibition as therapeutic strategies. |
| Molecular Formula |
C20H20O7
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|---|---|
| Molecular Weight |
372.3686
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| Exact Mass |
372.121
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| Elemental Analysis |
C, 64.51; H, 5.41; O, 30.08
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| CAS # |
945771-74-4
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| Related CAS # |
945771-96-0 (sodium); 945772-45-2 (free acid) |
| PubChem CID |
24786555
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| Appearance |
Beige fluffy powder
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| LogP |
3.712
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
499
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C2C(=C(C(=CC=2)OC)O)OC=1C)C1C=C(OC)C(OC)=C(OC)C=1
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| InChi Key |
RADMJHVVIZTENA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H20O7/c1-10-16(12-6-7-13(23-2)18(22)19(12)27-10)17(21)11-8-14(24-3)20(26-5)15(9-11)25-4/h6-9,22H,1-5H3
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| Chemical Name |
(7-hydroxy-6-methoxy-2-methyl-1-benzofuran-3-yl)-(3,4,5-trimethoxyphenyl)methanone
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| Synonyms |
BCN105; BCN 105; BCN-105
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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) |
DMSO: ~25 mg/mL (~67.1 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.71 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.71 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6855 mL | 13.4275 mL | 26.8550 mL | |
| 5 mM | 0.5371 mL | 2.6855 mL | 5.3710 mL | |
| 10 mM | 0.2686 mL | 1.3428 mL | 2.6855 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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