2. Cell Cycle/DNA Damage Autophagy Apoptosis
  3. DNA Alkylator/Crosslinker Autophagy Apoptosis
  4. Lomustine

Lomustine  (Synonyms: CCNU; NSC 79037)

Cat. No.: HY-13669 Purity: 99.90%
COA Handling Instructions

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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.

Lomustine Chemical Structure

Lomustine Chemical Structure

CAS No. : 13010-47-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 127 In-stock
Solution
10 mM * 1 mL in DMSO USD 127 In-stock
Solid
200 mg USD 115 In-stock
500 mg USD 226 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Lomustine:

Lomustine Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

DNA Alkylator[1]
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.

Lomustine Related Antibodies
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.
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 : 1 mg/mL (4.28 mM; ultrasonic and warming and heat to 60°C)

*"≥" 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
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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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%

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

Handling Instructions (2659 KB)
References
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

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
H2O / DMSO 1 mM 4.2790 mL 21.3950 mL 42.7899 mL 106.9748 mL
DMSO 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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