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^{[1][2][3][4][5][6]}.

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.

Cystemustine (35 mg/kg, i.v., single dose for 55 days) shows a large-amplitude diurnal rhythm toxicity variation with the lowest toxicity level of 15-19 hours after light onset (HALO) and highest level of 7 HALO^[2].
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.

257.70

C₆H₁₂ClN₃O₄S

79955-36-5

CS(CCNC(N(N=O)CCCl)=O)(=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]