Sarmustine

SKU: orb1699408

Description

Sarmustine

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 81965-43-7
• MW: 222.63
• Purity: 99.71%
• Formula: C₆H₁₁ClN₄O₃
• SMILES: C(N(CCCl)N=O)(N(CC(N)=O)C)=O
• Target: DNA Methyltransferase,DNA Alkylator/Crosslinker,p53,DNA Alkylation,Apoptosis
• Solubility: DMSO:50 mg/mL (224.59 mM)

Bioactivity

• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Sarmustine, Sarcosinamide, SarCNU, DNA alkylator, DNA Alkylation, DNAMethyltransferase, DNAAlkylation, DNA Methyltransferase, DNA methyltransferase (DNMT), NSC 364432, p53, NSC-364432, NSC364432

Compound Identifiers

PubChem CID

100773