Carmustine - CAS 154-93-8
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Not Intended for Therapeutic Use. For research use only.
DNA Alkylator/Crosslinker
Carmustine is  antineoplastic nitrosourea. Carmustine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis. This agent also carbamoylates proteins, including DNA repair enzymes, resulting in an enhanced cytotoxic effect. Carmustine is highly lipophilic and crosses the blood-brain barrier readily. Check for active clinical trials or closed clinical trials using this agent.
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bis(chloroethyl) nitrosourea; bis-chloronitrosourea; carmustin. Becenum; BiCNU; Carmubris. Becenun; Carmustinum; Nitrourean; Nitrumon. BCNU; FDA 0345; SK 27702; SRI 1720; WR-139021.
1.AN in vitro evaluation of a carmustine-loaded Nano-co-Plex for potential magnetic-targeted intranasal delivery to the brain.
Akilo OD1, Choonara YE1, Strydom AM2, du Toit LC1, Kumar P1, Modi G3, Pillay V4. Int J Pharm. 2016 Mar 16;500(1-2):196-209. doi: 10.1016/j.ijpharm.2016.01.043. Epub 2016 Jan 19.
Targeted delivery of carmustine (BCNU), an efficient brain tumor therapeutic, has been challenged with bioavailability issues due to the Blood Brain Barrier (BBB). The currently effective delivery approach is by implants at the site of the tumor, but this is highly invasive. The intranasal route, which is non-invasive and bypasses the BBB, may be alternative route for delivering BCNU to the brain. In this work, polyvinyl alcohol/polyethyleneimine/fIuorecein isothiocyanate complex (Polyplex) coated iron-oxide nanoparticles (Magnetite) were synthesized employing co-precipitation, epoxidation and EDC/NHS coupling reactions. The Polyplex coated magnetite (Nano-co-Plex) was loaded with BCNU for potential magnetically targeted delivery to the brain following intranasal administration. The Nano-co-Plex was characterized employing Thermogravimetric analysis (TGA), Superconducting Quantum Interference Device (SQUID) magnetometry, Fourier Transform Infrared Spectroscopy (FTIR), Nuclear Magnetic Resonance (NMR), X-ray Diffractometry (XRD), Transmission Electron Microscopy (TEM) and Zetasize analysis.
2.Combination Therapy with AKT3 and PI3KCA siRNA Enhances the Antitumor Effect of Temozolomide and Carmustine in T98G Glioblastoma Multiforme Cells.
Paul-Samojedny M1, Pudełko A2, Kowalczyk M3, Fila-Daniłow A3, Suchanek-Raif R3, Borkowska P3, Kowalski J3. BioDrugs. 2016 Apr;30(2):129-44. doi: 10.1007/s40259-016-0160-y.
BACKGROUND: Glioblastoma multiforme (GBM) is the most malignant and invasive human brain tumor, and it is characterized by a poor prognosis and short survival time. Current treatment strategies for GBM, using surgery, chemotherapy and/or radiotherapy, are ineffective. The PI3K/AKT/PTEN signaling pathway is frequently deregulated in this cancer, and it is connected with regulation of the cell cycle, apoptosis, and autophagy.
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