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Purity: ≥98%
Lomustine (also known as CCNU) is a nitrosourea anticancer drug that belongs to the class of DNA alkylating agents. Lomustine prevents the synthesis of DNA and RNA by alkylating and crosslinking DNA. Additionally, this agent carbamoylates proteins and DNA, which inhibits the synthesis of DNA and RNA and disrupts the processing of RNA. Because it is lipophilic, loxatine can pass through the blood-brain barrier.
| Targets |
DNA Alkylator
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|---|---|
| ln Vitro |
Lomustine inhibits ZR-75-1 and U373 from growing, with IC50 values of 12 μM and 15 μM, respectively. Lomustine inhibits the expression of O6-alkylguanine-DNA alkyltransferase, a DNA repair protein. [1] In both medulloblastoma and normal human epithelial and fibroblast cells, lomustine (420 μM) induces apoptosis via the mitochondrial pathway by lowering the levels of the anti-apoptosis proteins Bcl-2 and Bcl-xl, respectively. In medulloblastoma cells, locustrine causes a cell cycle delay in the G2/M phase; in HFSN1 cells, locustrine upregulates the level of the protein p21 in a p53-independent manner. [2]
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| ln Vivo |
Lomustine may result in irreversible, delayed, cumulative dose-related chronic hepatotoxicity that may be fatal. [4] In cats with spontaneously arising tumors, lomustine may occasionally cause severe hematological toxicity; grade III or IV neutropenia and thrombocytopenia have an incidence of 4.1% and 1.0%, respectively. In cats with spontaneously arising tumors, locustin tends to increase the risk of progressive neutropenia and statistically significant higher response rates. [5]
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| Cell Assay |
Cell lines are commonly grown as monolayers in DMEM supplemented with glutamine, penicillin/streptomycin, 10% foetal calf serum, and 25 mm HEPES. Studies on cytotoxicity are conducted in an atmosphere with 5% CO2 in a medium free of HEPES. In 96-well plates, 750–1000 cells/well are plated, and after an overnight incubation, they are treated for two hours either with or without 33 μM BG. In the same medium, temozolomide or CCNU is then added for an hour, with a final DMSO concentration of no more than 1%. Growth studies reveal that the cells are in log phase growth during the assay period. The cells are then cultured for an additional 7 days in fresh medium before being tested for protein content using the NCI sulphorhodamine assay. Cells are treated consecutively for 24 hours with fresh medium every day as part of the repeated temozolomide dosing schedule. At least two assays are performed.
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| Animal Protocol |
Mice: During the study, groups of eight B6C3F1 mice each receive PBS or 5-FC as the sole control. A single dose of 30 mg/kg of locustine is given to one group of mice (Lomustine Day 1 + PBS) on day 1, along with six cycles of PBS (800 μL/day, BID for four days in a row every ten days). For four days in a row, the remaining mice are given 5-FC (500 mg/kg/dose, IP, BID) along with either Lomustine on day one (Lomustine (CCNU) Day 1 + 5-FC) or Day 43 (Lomustine (CCNU) Day 43 + 5-FC for maximum benefit. Six cycles of four days on, ten days off, five FC, or five PBS are completed. When the final 5-FC treatment is completed, each experiment comes to an end. Every tissue is gathered and stored for pathology analysis.
Rats: Rat groups (n = 8 per group) are only given PBS or 5-FC as controls during the study. Rats in the Lomustine (CCNU) Day 1 + PBS group are given a single dose of 30 mg/kg of Lomustine on day 1 and six cycles of PBS (8 mL/day, BID). For five days in a row, the remaining rats are given 5-FC (500 mg/kg/dose, IP, BID) plus either Lomustine on Day 1 (Lomustine (CCNU) Day 1 + 5-FC) or Day 22 (Lomustine (CCNU) Day 22 + 5-FC), after which they are given two days off medication. A total of six repetitions of the 5-day on, 2-day off 5-FC or PBS cycle are made[3]. |
| References |
| Molecular Formula |
C9H16CLN3O2
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|---|---|
| Molecular Weight |
233.69524
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| Exact Mass |
233.09
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| Elemental Analysis |
C, 46.26; H, 6.90; Cl, 15.17; N, 17.98; O, 13.69
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| CAS # |
13010-47-4
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| Appearance |
Solid powder
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| SMILES |
C1CCC(CC1)NC(=O)N(CCCl)N=O
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| InChi Key |
GQYIWUVLTXOXAJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H16ClN3O2/c10-6-7-13(12-15)9(14)11-8-4-2-1-3-5-8/h8H,1-7H2,(H,11,14)
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| Chemical Name |
1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea
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| Synonyms |
NSC 79037; NSC-79037; NSC79037; Lomustinume. CeeNU; Belustin; Belustine; Cecenu; Citostal; Lomeblastin; Lucostin; Lucostine; Prava; CCNU; RB1509; WR139017
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 100 mg/mL (~427.9 mM)
H2O: < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30%propylene glycol+ 5%Tween 80+ 65%D5W, pH 4: 10.0mg/ml (42.79mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2790 mL | 21.3950 mL | 42.7899 mL | |
| 5 mM | 0.8558 mL | 4.2790 mL | 8.5580 mL | |
| 10 mM | 0.4279 mL | 2.1395 mL | 4.2790 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02796261 | Active Recruiting |
Drug: Eflornithine Drug: Lomustine |
Recurrent Anaplastic Astrocytoma Anaplastic Astrocytoma |
Orbus Therapeutics, Inc. | July 2016 | Phase 3 |
| NCT01682187 | Active Recruiting |
Drug: Lomustine Drug: LY2157299 |
Glioma | Eli Lilly and Company | December 15, 2005 | Phase 1 |
| NCT01582269 | Active Recruiting |
Drug: Lomustine Drug: Placebo |
Glioblastoma | Eli Lilly and Company | April 26, 2012 | Phase 2 |
| NCT05304663 | Not yet recruiting | Drug: Onfekafusp alfa Drug: Lomustine |
Glioblastoma | Philogen S.p.A. | June 1, 2022 | Phase 1 |
| NCT04573192 | Recruiting | Drug: Lomustine Drug: L19TNF |
Glioblastoma | Philogen S.p.A. | February 19, 2021 | Phase 1 Phase 2 |
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