Lomustine

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

For research use only.

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

Lomustine  Chemical Structure

CAS No. 13010-47-4

Selleck's Lomustine has been cited by 14 publications

Purity & Quality Control

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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]

Protocol (from reference)

Cell Research:[1]
  • 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.
Animal Research:[3]
  • Animal Models: Dogs
  • Dosages: 90 mg/m2
  • Administration: Orally

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 233.7
Formula

C9H16ClN3O2

CAS No. 13010-47-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCC(CC1)NC(=O)N(CCCl)N=O

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05304663 Not yet recruiting Drug: Onfekafusp alfa|Drug: Lomustine Glioblastoma Philogen S.p.A. June 1 2022 Phase 1
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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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