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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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BNC105 is a potent benzofuran-based tubulin polymerization inhibitor and also a vascular disrupting agent (VDA) prodrug with potential anti-vascular and anticancer activities. In vivo conditions cause a quick conversion of BNC105P to BNC105. By attaching itself to tubulin and preventing its polymerization, BNC105 can disrupt the tumor vasculature, stop the formation of mitotic spindles, and stop the cell cycle. Tumor cells experience apoptosis as a result of the ensuing hypoxic conditions, which starve them of nutrients. By blocking tubulin polymerization, this agent inhibits tumor cells directly in addition to its VDA activity. BNC105 is not a substrate for the multidrug-resistance P-glycoprotein (Pgp) transporter.
References |
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Molecular Formula |
C20H20O7
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Molecular Weight |
372.3686
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Exact Mass |
372.12
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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) |
Appearance |
Beige fluffy powder
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SMILES |
CC1=C(C2=C(O1)C(=C(C=C2)OC)O)C(=O)C3=CC(=C(C(=C3)OC)OC)OC
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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.
BNC105P and targeted therapy treatment suppresses vasculature recovery in MDA-MB-231 xenograft. Cancer Biol Ther . 2014;15(11):1552-60 td> |
Molecular and cellular events associated with BNC105 induced vascular disruption and tumor recovery. Cancer Biol Ther . 2014;15(11):1552-60 td> |
measurement of the activity of BNC105, two chemically related compounds (0075 and 0079), CA4, paclitaxel, vinblastine, and vincristine on the proliferation of activated and quiescent HUVEC and HAAEC. EC50 values are based on three replicates obtained following a 48-h exposure to increasing doses of compound. Mol Cancer Ther . 2010 Jun;9(6):1562-73. td> |
BNC105 selectively inhibits the formation of endothelial cell capillaries but does not affect preformed capillaries. Mol Cancer Ther . 2010 Jun;9(6):1562-73. td> |