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 individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W, pH 4
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03022578||Not yet recruiting||Malignant Neoplasms of Eye Brain and Other Parts of Central Nervous System|Glioblastoma|Anaplastic Astrocytoma||M.D. Anderson Cancer Center|Monteris Medical||May 2017||Phase 2|
|NCT02986178||Not yet recruiting||Malignant Glioma||Darell D. Bigner, MD, PhD|Duke University||March 2017||Phase 2|
|NCT03025893||Not yet recruiting||Glioblastoma Multiforme|Glioblastoma, Adult|Glioblastoma|Recurrent Brain Tumor|GBM||VU University Medical Center||March 2017||Phase 2|Phase 3|
|NCT02724579||Not yet recruiting||Untreated Childhood Medulloblastoma||Childrens Oncology Group|National Cancer Institute (NCI)||October 2016||Phase 2|
|NCT01775475||Recruiting||AIDS-related Diffuse Large Cell Lymphoma|AIDS-related Diffuse Mixed Cell Lymphoma|AIDS-related Diffuse Small Cleaved Cell Lymphoma|AIDS-related Immunoblastic Large Cell Lymphoma|AIDS-related Lymphoblastic Lymphoma|AIDS-related Peripheral/Systemic Lymphoma|AIDS-related Small Noncleaved Cell Lymphoma|Stage III AIDS-related Lymphoma|Stage IV AIDS-related Lymphoma||AIDS Malignancy Consortium|National Cancer Institute (NCI)|The EMMES Corporation||September 2016||Phase 2|
|NCT02843230||Not yet recruiting||Glioblastoma||Massachusetts General Hospital||August 2016||--|
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