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Lomustine DNA/RNA Synthesis chemical

Name: Lomustine
Brand: Selleck Chemicals
SKU: S1840
Availability: InStock
Rating: 5 (21 reviews)

Cat.No.S1840

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

Chemical Structure

Molecular Weight: 233.7

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.89%

99.89

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Chemical Information, Storage & Stability

Molecular Weight	233.7	Formula	C₉H₁₆ClN₃O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	13010-47-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC79037, Gleostine, CeeNU, CCNU			Smiles	C1CCC(CC1)NC(=O)N(CCCl)N=O

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W, pH 4 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (42.79mM)	Taking the 1 mL working solution as an example, add 300 μL of clarified propylene glycol stock solution of 33.33 mg/ml to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W, pH 4, to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

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. This compound reduces the level of expression of the DNA repair protein O6-alkylguanine-DNA alkyltransferase. ^[1] It (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. This chemical 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] This compound 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. It trends toward a greater likelihood for progressive neutropenia and statistically significant higher response rates in cats with spontaneously arising tumors. ^[5]
References	https://pubmed.ncbi.nlm.nih.gov/8512814/ https://pubmed.ncbi.nlm.nih.gov/18058069/ https://pubmed.ncbi.nlm.nih.gov/10587263/ https://pubmed.ncbi.nlm.nih.gov/14765735/ https://pubmed.ncbi.nlm.nih.gov/12118689/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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