For research use only.

Catalog No.S1840 Synonyms: NSC79037, Gleostine, CeeNU, CCNU

8 publications

Lomustine  Chemical Structure

CAS No. 13010-47-4

Lomustine (NSC79037, Gleostine, CeeNU, CCNU) inhibits cancer cells by damaging the DNA and stops cells from dividing.

Selleck's Lomustine has been cited by 8 publications

1 Customer Review

  • Initial range finding concentration response analysis of the cytotoxic effects of (A) lomustine (IC50 = 12 μM) and (B) vincristine (IC50 = 1.5 nM) on D283 Med in a clonogenic assay of cell survival

    J Cell Mol Med, 2017, 21(12):3337-3346. Lomustine purchased from Selleck.

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Biological Activity

Description Lomustine (NSC79037, Gleostine, CeeNU, CCNU) inhibits cancer cells by damaging the DNA and stops cells from dividing.
Features A more specific and potent anti-medulloblastoma agent compared to Vincristine.
In vitro

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. [1] 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. [2]

In vivo Lomustine can cause delayed, cumulative dose-related, chronic hepatotoxicity that is irreversible and can be fatal. [4] 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. [5]


Cell Research:[1]
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  • Cell lines: XP cells
  • Concentrations: 133 μM
  • Incubation Time: 1 hour
  • Method: Cell lines are routinely grown as monolayers in DMEM supplemented with 10% foetal calf serum, 25 mm HEPES, glutamine and penicillin/streptomycin. Cytotoxicity studies are carried out in HEPES-free medium in a 5% CO2 atmosphere. 750-1000 cells/well are plated in 96 well plates and after overnight incubation are treated for 2 hours with or without 33 μM BG. Temozolomide or CCNU is then added for 1 hour in the same medium, the final DMSO concentration not exceeding 1%. The cells are grown for a further 7 days in fresh medium and assayed for protein content by the NCI sulphorhodamine assay; growth studies show that cells are in log phase growth during the assay period. For the repeat temozolomide dosing schedule cells are given consecutive 24 hours treatments, with fresh medium each day. Assays are carried out at least in duplicate.
    (Only for Reference)
Animal Research:[3]
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  • Animal Models: Dogs
  • Dosages: 90 mg/m2
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 46 mg/mL (196.83 mM)
Water Insoluble
Ethanol Insoluble
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.
10 mg/mL

* 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.

Chemical Information

Molecular Weight 233.7


CAS No. 13010-47-4
Storage powder
in solvent
Synonyms NSC79037, Gleostine, CeeNU, CCNU
Smiles C1CCC(CC1)NC(=O)N(CCCl)N=O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01989052 Terminated Drug: CTO|Drug: Lomustine Malignant Glioma (WHO Grade III or IV) Annick Desjardins|Tactical Therapeutics Inc.|Duke University May 2014 Phase 1
NCT01562197 Completed Drug: axitinib|Drug: Axitinib plus Lomustine Glioblastoma Multiforme Bart Neyns|Pfizer|Universitair Ziekenhuis Brussel April 2014 Phase 2
NCT01149109 Completed Drug: Temozolomide and lomustine|Drug: Temozolomide Glioblastoma University Hospital Bonn October 2010 Phase 3
NCT00503204 Completed Drug: Cediranib|Drug: Lomustine Recurrent Glioblastoma|Brain Tumor AstraZeneca September 2007 Phase 1
NCT00295815 Completed Drug: enzastaurin|Drug: lomustine Glioblastoma Eli Lilly and Company January 2006 Phase 3

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DNA/RNA Synthesis Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID