| Name | Sarmustine |
| Description | Sarmustine (SarCNU) is an alkylating agent with anticancer activity that inhibits the growth of prostate cancer cells via p53-dependent and p53-independent pathways.Sarmustine mediates the selection of P140K methylguanine-DNA-methyltransferase-transduced human CD34(+) cells in vitro. |
| In vivo | Sarmustine (SarCNU) (s.c.) implanted SF-295 and U-251 central nervous system (CNS) tumor xenografts. When given i.v., q4d for 3 doses, to athymic mice bearing s.c. SF-295 tumors, SarCNU, at an optimum of 167 mg/kg/dose, produced 9 tumor-free animals of 10 total animals, 1 regression, and no evidence of overt toxicity (> or =20% body weight loss). Furthermore, SarCNU retained high antitumor activity at two lower dose levels, 66 and 45% of the optimal dose, whereas BCNU demonstrated a progressive loss of antitumor activity at lower doses. Following p.o. administration, SarCNU similarly demonstrated antitumor activity. In the U-251 CNS tumor model, SarCNU yielded six of six tumor-free animals at 80 mg/kg/dose with i.p. administration q.d. for 5 days, starting on day 14, whereas BCNU, at 9 mg/kg/dose, yielded three of six tumor-free mice and one drug-related death. Again, SarCNU resulted in tumor-free animals at 66 and 45% of its optimal dose and was relatively nontoxic. Results of testing to date indicate that SarCNU is clearly more effective than BCNU against the human CNS tumors SF-295 and U-251 in vivo. These results encourage the initiation of clinical trials for SarCNU, in an effort to improve therapeutic approaches to glioma.[3] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (224.59 mM), Sonication is recommended.
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| Keywords | Sarmustine | p53 | DNAMethyltransferase | DNAAlkylation | DNA methyltransferase (DNMT) | DNA Methyltransferase | DNA alkylator | DNA Alkylation |
| Inhibitors Related | Stavudine | Aceglutamide | Tamoxifen | Urea | Cysteamine hydrochloride | Gum arabic | Sodium 4-phenylbutyrate | Metronidazole | Citric Acid Triammonium | Dimethyl phthalate | Alginic acid | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Apoptosis Compound Library | DNA Damage & Repair Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | ReFRAME Related Library | HIF-1 Signaling Pathway Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | Transcription Factor-Targeted Compound Library |
United States
