Lomustine
Based on 7 publication(s) in Google Scholar
Lomustine (CCNU; NSC 79037) is a DNA alkylating agent, with antitumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.90%
- No. CAS: 13010-47-4
- Fòrmula: C9H16ClN3O2
- Peso molecular:233.70
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Lomustine
More- Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
- Int J Oncol. 2022 Nov;61(5):139. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Diagnostics (Basel). 2023 Mar 24;13(7):1232. [Abstract]
- Mol Imaging Biol. 2020 Feb;22(1):124-133. [Abstract]
- bioRxiv. 2023 Jul 17.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
Actividad biológica
Descripciòn
IC50 & Target
DNA Alkylator[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L1210 | ED50 |
37 mg/kg
Compound: Table III, R1C1
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Antitumor activity against mouse L1210 cells allografted in ip dosed BDF1 mouse assessed as increase of life span of host measured up to 45 days
Antitumor activity against mouse L1210 cells allografted in ip dosed BDF1 mouse assessed as increase of life span of host measured up to 45 days
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[PMID: 836500] |
| P388 | ED50 |
13 μM
Compound: CCNU
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Mean value for the exposure for P388 to the drug for a period of 60 min
Mean value for the exposure for P388 to the drug for a period of 60 min
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[PMID: 6226795] |
| P388 | ED50 |
6.7 μM
Compound: CCNU
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Mean value for the exposure for P388 to the drug for a period of 40 min at pH 7.4 and 37 degree
Mean value for the exposure for P388 to the drug for a period of 40 min at pH 7.4 and 37 degree
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[PMID: 6226795] |
In Vitro
Lomustine (CCNU; NSC 79037) is a DNA alkylating agent. Lomustine (CCNU, 0-250 μM) is cytotoxic to the U87-MG cells expressing tumor-derived mutant IDH1, and has little effect on the expression of wild-type IDH1. The combination of Lomustine and procarbazine or vincristine has no additive effect on the killing of cells expressing mutant or wild-type IDH1. Moreover, overexpression of either ALKBH2 or ALKBH3 partially reduces the death HT1080 cells exposed to Lomustine[1]. Lomustine (CCNU) suppresses U87-MG growth with an ED50 of 68.1 μM. Lomustine (CCNU) (30, 40 μM) in combination with docosahexaenoic acid (DHA) darmatically inhibits 2 additional human-derived glioblastoma cell lines, and induces U87-MG apoptosis and necrosis. Lomustine (30 μM) causes G2/M arrest[2]. Lomustine (CCNU) reduces the viability of F98 rat orthotopic glioma cells and Tu-2449 mouse glioma cell line, with IC50s of 20.8 μM and 18.6 μM, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 13010-47-4
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Appearance Solid
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Peso molecular 233.70
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Fòrmula C9H16ClN3O2
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Color Light yellow to yellow
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SMILES
O=C(NC1CCCCC1)N(CCCl)N=O
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Synonyms
CCNU; NSC 79037
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
Int J Oncol
2022 Nov;61(5):139. PMID: 36169178 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Diagnostics (Basel)
Application of Drug Testing Platforms in Circulating Tumor Cells and Validation of a Patient-Derived Xenograft Mouse Model in Patient with Primary Intracranial Ependymomas with Extraneural Metastases. [Abstract]2023 Mar 24;13(7):1232. PMID: 37046450 -
Mol Imaging Biol
Evaluation of Glycolytic Response to Multiple Classes of Anti-glioblastoma Drugs by Noninvasive Measurement of Pyruvate Kinase M2 Using [18F]DASA-23. [Abstract]2020 Feb;22(1):124-133. PMID: 30989436
Lomustine purchased from MedChemExpress. Usage Cited in: Mol Imaging Biol. 2020 Feb;22(1):124-133. [Abstract]
Three-day treatment; untreated vs temozolomide, ***p = 0.0004; untreated vs carmustine, ****p < 0.0001; untreated vs lomustine, **p = 0.002; untreated vs procarbazine, ****p < 0.0001; n = 6 per condition, p values obtained from one-way ANOVA with Bonferroni correction for multiple comparisons.
Lomustine purchased from MedChemExpress. Usage Cited in: Mol Imaging Biol. 2020 Feb;22(1):124-133. [Abstract]
Six-day treatment; untreated vs temozolomide, ****p < 0.0001; untreated vs carmustine, ****i < 0.0001; untreated vs lomustine, ****p < 0.0001; untreated vs procarbazine, ****p < 0.0001; n = 6 per condition, p values obtained from one-way ANOVA with Bonferroni correction for multiple comparisons.
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Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (427.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Cell Assay[2]
Initially, cells (5000 cells/well) are cultured in 96-well flat-bottom plates overnight in complete medium to establish a linear growth rate. Spent medium is replaced with new medium supplemented with 2% FBS and varying treatments (100 μL total volume/well). Ethanol-supplemented cells (< 0.5%) serve as the vehicle control. Cells are maintained at 37°C in 5% CO2 in a humidified atmosphere for 24 hours prior to assessment of cell growth with the WST-1 assay reagent. Medium alone combined with the WST-1 assay reagent establishes nonspecific values that are subtracted from the experimental optical density (OD) readings (OD at 450 nm). Vehicle control OD readings serve as standard proliferative potential normalized to 100%. The proliferation index is calculated by dividing the average OD treatment reading by the average OD vehicle reading and multiplying by 100[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[3]
Mice[3]
Groups of B6C3F1 mice receive PBS or 5-FC only as a control during the study (n = 8 per group). One group of mice (Lomustine Day 1 + PBS) receive one dose of Lomustine (30 mg/kg) on day 1 and a total of six cycles of PBS (800 μL/day, BID for 4 consecutive days every 10 days). The rest of the mice receive 5-FC (500 mg/kg/dose, IP, BID) for 4 consecutive days, plus Lomustine at day 1 (Lomustine (CCNU) Day 1 + 5-FC) or day 43 (Lomustine (CCNU) Day 43 + 5-FC). Cycles of 4-days on, 10-days off 5-FC or PBS are repeated a total of 6 times. Each experiment is terminated at the end of the last 5-FC treatment. All tissues are collected and saved for histopathology. Toxicity in groups receiving Lomustine is compared to the groups receiving PBS or 5-FC alone or in combination with 5-FC at designated time points[3].
Rats[3]
Groups of rats receive PBS or 5-FC only as controls during the study (n = 8 per group). One group of rats (Lomustine (CCNU) Day 1 + PBS) receive one dose of Lomustine (30 mg/kg) at day 1 and a total of six cycles of PBS (8 mL/day, BID). The rest of the rats receive 5-FC (500 mg/kg/dose, IP, BID) for 5 consecutive days, followed by 2 days off drug, plus Lomustine on day 1 (Lomustine (CCNU) Day 1 + 5-FC) or day 22 (Lomustine (CCNU) Day 22 + 5-FC). Cycles of 5-days on, 2-days off 5-FC or PBS are repeated a total of 6 times[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wang P, et al. Oncometabolite D-2-Hydroxyglutarate Inhibits ALKBH DNA Repair Enzymes and Sensitizes IDH Mutant Cells to Alkylating Agents. Cell Rep. 2015 Dec 22;13(11):2353-2361. [Content Brief]
[2]. Harvey KA, et al. Enhanced anticancer properties of lomustine in conjunction with docosahexaenoic acid in glioblastoma cell lines. J Neurosurg. 2015 Mar;122(3):547-56. [Content Brief]
[3]. Yagiz K, et al. Toca 511 plus 5-fluorocytosine in combination with lomustine shows chemotoxic and immunotherapeutic activity with no additive toxicity in rodent glioblastoma models. Neuro Oncol. 2016 Oct;18(10):1390-401. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.2790 mL | 21.3950 mL | 42.7899 mL | 106.9748 mL |
| 5 mM | 0.8558 mL | 4.2790 mL | 8.5580 mL | 21.3950 mL | |
| 10 mM | 0.4279 mL | 2.1395 mL | 4.2790 mL | 10.6975 mL | |
| 15 mM | 0.2853 mL | 1.4263 mL | 2.8527 mL | 7.1317 mL | |
| 20 mM | 0.2139 mL | 1.0697 mL | 2.1395 mL | 5.3487 mL | |
| 25 mM | 0.1712 mL | 0.8558 mL | 1.7116 mL | 4.2790 mL | |
| 30 mM | 0.1426 mL | 0.7132 mL | 1.4263 mL | 3.5658 mL | |
| 40 mM | 0.1070 mL | 0.5349 mL | 1.0697 mL | 2.6744 mL | |
| 50 mM | 0.0856 mL | 0.4279 mL | 0.8558 mL | 2.1395 mL | |
| 60 mM | 0.0713 mL | 0.3566 mL | 0.7132 mL | 1.7829 mL | |
| 80 mM | 0.0535 mL | 0.2674 mL | 0.5349 mL | 1.3372 mL | |
| 100 mM | 0.0428 mL | 0.2139 mL | 0.4279 mL | 1.0697 mL |
Lomustine Related Classifications
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