A DNA alkylating agent
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].
参考文献:
[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]: | |
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Cell lines |
L1210 leukemia cells |
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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. |
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Reacting condition |
50 μg/ml, 37°C |
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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]: | |
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Animal models |
L1210 leukemia-bearing mice |
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Dosage form |
0.5 mg in 0.2 ml of dimethyl sulfoxide; i.p. injection |
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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. |
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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. |
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参考文献: [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. | |
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