Lomustine (Synonyms: CCNU; NSC 79037)

Name: Lomustine
Brand: MedChemExpress
SKU: HY-13669
Rating: 5.0 (6 reviews)

Cat. No.: HY-13669 Purity: 99.90%: Data Sheet
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Lomustine (CCNU; NSC 79037) is a DNA alkylating agent, with antitumor activity.

For research use only. We do not sell to patients.

CAS No. : 13010-47-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
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5 g	Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Lomustine:

Lomustine (Standard) In-stock

6 Publications Citing Use of MCE Lomustine

Cell Proliferation/Viability Assay

: 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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Biological Activity
Protocol
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Description

Lomustine (CCNU; NSC 79037) is a DNA alkylating agent, with antitumor activity.

IC₅₀ & Target

DNA Alkylator^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
L1210	ED₅₀	37 mg/kg Compound: Table III, R1C1	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	[PMID: 836500]
P388	ED₅₀	13 μM Compound: CCNU	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	[PMID: 6226795]
P388	ED₅₀	6.7 μM Compound: CCNU	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	[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

Lomustine (CCNU; NSC 79037) (30 mg/kg) in combination with Toca 511 + 5-FC prolongs survival in rats bearing F98 tumor cells. Lomustine (CCNU) (30 mg/kg) combined with Toca-511 + 5-FC also exhibits antitumor activity in the B6C3F1 mice bearing Tu-2449 glioma cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

233.70

Formula

C₉H₁₆ClN₃O₂

CAS No.

13010-47-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1CCCCC1)N(CCCl)N=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (10.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (279 KB) SDS (644 KB)

COA (245 KB) HNMR (249 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lomustine13010-47-4CCNU NSC 79037NSC79037NSC 79037NSC-79037DNA Alkylator/CrosslinkerAutophagyApoptosisInhibitorinhibitorinhibit

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Lomustine (Synonyms: CCNU; NSC 79037)

Customer Review

Other Forms of Lomustine:

Lomustine Related Antibodies

6 Publications Citing Use of MCE Lomustine

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Lomustine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Lomustine Related Classifications

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