Lomustine (Synonyms: CCNU, NCI C04740, NSC 79037) |
| Catalog No.GC17865 |
Antineoplastic drug
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 13010-47-4
Sample solution is provided at 25 µL, 10mM.
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Lomustine is an antineoplastic drug used in chemotherapy [1]
Lomustine has been revealed to inhibit the growth of tumour cell lines with IC50 values of 25μM, 8.8μM and 13μM for breast ZR-75-1, astrocytoma U87MG and colorectal LS174T cell lines [2]. Besides, Lomustine has been found to be particularly effective in the treatment of certain neoplasms of the central nervous system, because of the high lipid solubility and permeability through the blood brain barrier. In addition, Lomustine has shown the effect function in treatment of meningeal leukemia in the mouse and in children who have acute leukemia with central nervous system involvement [1].
References:
[1] Cheng CJ, Fujimura S, Grunberger D, Weinstein IB. nteraction of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (NSC 79037) with nucleic acids and proteins in vivo and in vitro. Cancer Res. 1972 Jan;32(1):22-7.
[2] Baer JC1, Freeman AA, Newlands ES, Watson AJ, Rafferty JA, Margison GP. Depletion of O6-alkylguanine-DNA alkyltransferase correlates with potentiation of temozolomide and CCNU toxicity in human tumour cells.Br J Cancer. 1993 Jun; 67(6):1299-302.
| Cell experiment [1]: | |
|
Cell lines |
L1210 leukemia cells |
|
Preparation method |
The solubility of this compound in DMSO is >11.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
50 μg/ml, 37°C |
|
Applications |
In L1210 leukemia cells, the radioactivity of the cyclohexyl moiety of CCNU (Lomustine) was bound almost exclusively to proteins, and that of the ethylene group was bound (at a much lower level) to both nucleic acids and proteins. |
| Animal experiment [1]: | |
|
Animal models |
L1210 leukemia-bearing mice |
|
Dosage form |
0.5 mg in 0.2 ml of dimethyl sulfoxide; i.p. injection |
|
Application |
In L1210 leukemia-bearing mice, the radioactivity of the cyclohexyl moiety of CCNU (Lomustine) was almost exclusively bound to cellular proteins, rather than to nucleic acids. The radioactivity of the ethylene moiety was bound to both nucleic acids and proteins of brain, liver, and leukemia cells to about the same level. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1] Cheng CJ, Fujimura S, Grunberger D, Weinstein IB. Interaction of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (NSC 79037) with nucleic acids and proteins in vivo and in vitro. Cancer Res. 1972 Jan;32(1):22-7. | |
| Cas No. | 13010-47-4 | SDF | |
| Synonyms | CCNU, NCI C04740, NSC 79037 | ||
| Chemical Name | 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea | ||
| Canonical SMILES | C1CCC(CC1)NC(=O)N(CCCl)N=O | ||
| Formula | C9H16ClN3O2 | M.Wt | 233.7 |
| Solubility | ≥ 11.7mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.279 mL | 21.395 mL | 42.7899 mL |
| 5 mM | 0.8558 mL | 4.279 mL | 8.558 mL |
| 10 mM | 0.4279 mL | 2.1395 mL | 4.279 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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