Cystemustine
Cystemustine is a DNA inhibitor (a chloroethyl nitrosourea, CENU). Cystemustine can cause DNA cross-linking, thereby inhibiting the proliferation of tumor cells. Cystemustine can also exert cytotoxic effects by interfering with the cell cycle, inducing cell re-differentiation, and altering phospholipid metabolism. Cystemustine exhibits high anti-tumor activity and a relatively short plasma half-life in mice. Cystemustine can be used for the study of various malignant tumors, including melanoma, glioma, renal cancer, head and neck cancer, and colorectal cancer, etc.
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- No. CAS: 79955-36-5
- Fòrmula: C6H12ClN3O4S
- Peso molecular:257.70
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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- Referencias
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Actividad biológica
Descripciòn
In Vitro
Cystemustine (100, 200 μM, 2 h) causes no significant DNA damage alone, but combination with O6-benzyl-N2-acetylguanosine (BNAG) significantly increases DNA lesions in M3Dau cells[3].
Cystemustine (50 μM, 4 h) causes cytotoxicity causes cytotoxicity in M4Beu cells, but its effect is enhanced when combined with lGgBZ (an O6-alkylguanine-DNA alkyltransferase inhibitor)[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:M3Dau cells
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Concentration:100, 200 μM or with BNAG (300 μM)
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Incubation Time:2 h or after 4 h
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Result:Did not significantly modify the level of amplification of the DNA fragment alone.
Caused 1.85 or 2.55 injuries respectively with combined with BNAG.
In Vivo
Cystemustine (15 mg/kg, i.v. or injected directly into the tumor, at days 1-19) induces deep alterations concerning cell morphology, cell cycle, and melanin content in melanoma mice model[4].
Cystemustine (15 mg/kg, injected directly into the tumor, at days 11-18) makes melanoma tumors a new phospholipid metabolism phenotype in mice model[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Active span of the rest-activity circadian cycle in male B6DZFI mice (9-10 weeks)[2]
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Dosage:35 mg/kg
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Administration:Intravenous injection (i.v.), single dose for 55 days
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Result:Survival rate ranged from only 3.8% at HALO up to 87.5 and 88.2% at 15 and 19 HALO, respectively.
Weight loss ranged from -16.6% at 15 HALO to -27.3% at 3 HALO.
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Animal Model:Melanoma model established in male C57BL6/6J mice, 6-8 weeks[4]
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Dosage:15 mg/kg
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Administration:Intravenous injection (i.v.) or injected directly into the tumor (i.t.), at days 1, 5, and 9 after B16 cell inoculation or at days 11, 14, and 19 after inoculation
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Result:Exhibited alteration in cell morphology and increase in melanin content.
Strongly reduced the number of mitoses/microscopic field by 10-fold.
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Animal Model:Melanoma model established in male C57BL6/6J mice, 6-8 weeks[5]
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Dosage:15 mg/kg
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Administration:Injected directly into the tumor (i.t.), at days 11, 14, and 18 from B16 cell inoculation
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Result:Induced a sustained redifferentiation pattern.
Exhibited transient increase in Cho, GPC, and GPE and sustained elevation of PC and PE during growth inhibition.
Exhibited sustained overexpression of PC and PE during growth recovery.
Chemical Information
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No. CAS 79955-36-5
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Peso molecular 257.70
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Fòrmula C6H12ClN3O4S
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SMILES
CS(CCNC(N(N=O)CCCl)=O)(=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Palmer B. Cystemustine INSERM. IDrugs. 1998 May;1(1):129-35. PMID: 18465517. [Content Brief]
[2]. Martineau-Pivoteau N, et al. Circadian rhythm in toxic effects of cystemustine in mice: relevance for chronomodulated delivery. Int J Cancer. 1996 Nov 27;68(5):669-74. [Content Brief]
[3]. Buchdahl C, et al. Melanoma-cell toxicity of cystemustine combined with O6-benzyl-N2-acetylguanosine. Melanoma Res. 1998 Apr;8(2):123-30. [Content Brief]
[4]. Demidem A, et al. Cystemustine induces redifferentiation of primary tumors and confers protection against secondary tumor growth in a melanoma murine model. Cancer Res. 2001 Mar 1;61(5):2294-300. [Content Brief]
[5]. Morvan D,et al. Melanoma tumors acquire a new phospholipid metabolism phenotype under cystemustine as revealed by high-resolution magic angle spinning proton nuclear magnetic resonance spectroscopy of intact tumor samples. Cancer Res. 2002 Mar 15;62(6):1890-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cystemustine Related Classifications
HY-106435 Related Classifications
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