Home DNA Damage/DNA Repair DNA/RNA Synthesis chemical Lomustine For research use only.

Lomustine

Synonyms: NSC79037, Gleostine, CeeNU, CCNU

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

Lomustine Chemical Structure

Lomustine Chemical Structure

CAS No. 13010-47-4

Purity & Quality Control

Lomustine Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Dogs
Dosages 90 mg/m2
Administration Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05904119 Recruiting
First Progression of Glioblastoma
European Organisation for Research and Treatment of Cancer - EORTC
 March 15 2024 Phase 3
NCT05304663 Withdrawn
Glioblastoma
Philogen S.p.A.
 June 1 2022 Phase 1
NCT01989052 Terminated
Malignant Glioma (WHO Grade III or IV)
Annick Desjardins|Tactical Therapeutics Inc.|Duke University
 May 2014 Phase 1
NCT01562197 Completed
Glioblastoma Multiforme
Bart Neyns|Pfizer|Universitair Ziekenhuis Brussel
 April 2014 Phase 2
NCT01149109 Completed
Glioblastoma
University Hospital Bonn
 October 2010 Phase 3

Chemical Information & Solubility

Molecular Weight 233.7 Formula

C9H16ClN3O2
CAS No. 13010-47-4 SDF Download Lomustine SDF
Smiles C1CCC(CC1)NC(=O)N(CCCl)N=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 47 mg/mL ( (201.11 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

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.

Handling Instructions

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