BNC-105

• CAS: 945771-74-4
• Catalog Number: ACM945771744
• Category: Inhibitors
• Molecular Weight: 372.37
• Molecular Formula: C20H20O7
• Description: BNC105 is a novel compound being developed by Bionomics as a Vascular Disrupting Agent (VDA) for treatment of cancer. VDAs are drugs that disrupt the blood vessels that nourish tumours. BNC105 acts as a tubulin polymerization inhibitor and displays 80-fold higher potency against endothelial cells than that of CA4P. CA4P is a VDA currently under evaluation in phase III clinical trials. BNC105 is more potent and offers a wider therapeutic window. CA4P produces 90% vascular disruption at its no observed adverse event level (NOAEL), whereas BNC105 causes 95% vascular disruption at 1/8th of its NOAEL. Tissue distribution analysis of BNC105 in tumor-bearing mice showed that while the drug is cleared from all tissues 24 hours after administration, it is still present at high concentrations within the solid tumor mass. Furthermore, BNC105 treatment causes tumor regressions with complete tumor clearance in 20% of treated animals.
• Synonyms: BCN105; BCN-105; BCN 105
• IUPAC Name: (7-hydroxy-6-methoxy-2-methylbenzofuran-3-yl)(3,4,5-trimethoxyphenyl)methanone
• Canonical SMILES: O=C(C1=C(C)OC2=C(O)C(OC)=CC=C12)C3=CC(OC)=C(OC)C(OC)=C3
• InChI: 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
• InChI Key: RADMJHVVIZTENA-UHFFFAOYSA-N
• Solubility: Soluble in DMSO, not in water
• Appearance: Beige fluffy powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 64.51; H, 5.41; O, 30.08
• Exact Mass: 372.1209
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: BNC105 exhibits an EC50 for chromatin condensation of <20 nmol/L, while vinblastine and CA4 demonstrated EC50 ≥ 100 nmol/L. The ability of these drugs to impact the biomarkers phospho-JNK and Noxa correlated with apoptosis. BNC105 was ~10x more potent than vinblastine and CA4 to activate JNK and Noxa and induce apoptosis (Fig. 1A).; Reference: Cancer Biol Ther. 2016 Mar; 17(3): 291-299. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4847999/
• In Vivo Activity: BNC105 is more potent and offers a wider therapeutic window. CA4 produces 90% vascular disruption at its no observed adverse event level (NOAEL), whereas BNC105 causes 95% vascular disruption at 1/8th of its NOAEL. Tissue distribution analysis of BNC105 in tumor-bearing mice showed that while the drug is cleared from all tissues 24 hours after administration, it is still present at high concentrations within the solid tumor mass. Furthermore, BNC105 treatment causes tumor regressions with complete tumor clearance in 20% of treated animals.; Reference: J Med Chem. 2011 Sep 8; 54(17): 6014-6027. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3172808/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).