Catalog No.S1840 Synonyms: nsc79037
Molecular Weight(MW): 233.7
Lomustine inhibits cancer cells by damaging the DNA and stops cells from dividing.
Purity & Quality Control
Choose Selective DNA/RNA Synthesis Inhibitors
|Description||Lomustine inhibits cancer cells by damaging the DNA and stops cells from dividing.|
|Features||A more specific and potent anti-medulloblastoma agent compared to Vincristine.|
Lomustine inhibits the growth of ZR-75-1 and U373 with IC50 of 12 μM and 15 μM, respectively. Lomustine reduces the level of expression of the DNA repair protein O6-alkylguanine-DNA alkyltransferase.  Lomustine (420 μM) triggers apoptosis through the mitochondrial pathway via decrease in the level of the anti-apoptosis proteins Bcl-2 and Bcl-xl, respectively, in both medulloblastoma and normal human epithelial and fibroblast cells. Lomustine induces cell cycle delay in G2/M phase in medulloblastoma cells and up-regulates p21 protein level in a p53-independent manner in HFSN1 cells. 
|In vivo||Lomustine can cause delayed, cumulative dose-related, chronic hepatotoxicity that is irreversible and can be fatal.  Lomustine could result in infrequent severe hematological toxicity in cats with spontaneously arising tumors, and the incidence of either grade III or IV neutropenia and thrombocytopenia is 4.1% and 1.0%, respectively. Lomustine trends toward a greater likelihood for progressive neutropenia and statistically significant higher response rates in cats with spontaneously arising tumors. |
-  Baer JC, et al. Br J Cancer, 1993, 67(6), 1299-12302.
-  Shinwari Z, et al. J Neurooncol, 2008, 87(2), 123-132.
-  Rassnick KM, et al. J Vet Intern Med, 1999, 13(6), 601-605.
|In vitro||DMSO||46 mg/mL (196.83 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W, pH 4
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03022578||Recruiting||Malignant Neoplasms of Eye Brain and Other Parts of Central Nervous System|Glioblastoma|Anaplastic Astrocytoma||M.D. Anderson Cancer Center|Monteris Medical||November 7 2017||Phase 2|
|NCT03025893||Recruiting||Glioblastoma Multiforme|Glioblastoma Adult|Glioblastoma|Recurrent Brain Tumor|GBM||VU University Medical Center||August 31 2018||Phase 2|Phase 3|
|NCT01934361||Completed||Recurrent Glioblastoma Multiforme||Novartis Pharmaceuticals|Novartis||February 28 2014||Phase 1|
|NCT03149575||Active not recruiting||Glioblastoma Multiforme|Glioblastoma|Glioma|GBM|Brain Cancer||DelMar Pharmaceuticals Inc.||October 27 2017||Phase 3|
|NCT02796261||Recruiting||Anaplastic Astrocytoma|Recurrent Anaplastic Astrocytoma||Orbus Therapeutics Inc.||July 2016||Phase 3|
|NCT02765165||Active not recruiting||Solid Tumors (Phase 1)|Relapsed/Recurrent GBM (Phase 2)||Proximagen LLC||April 2016||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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