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Sarmustine

Catalog No. T28663 CAS 81965-43-7

Synonyms: NSC-364432, SarCNU, Sarcosinamide, NSC 364432, NSC364432

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.

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Sarmustine, CAS 81965-43-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 195.00
5 mg	In stock	$ 483.00
10 mg	In stock	$ 692.00
25 mg	In stock	$ 1,080.00
50 mg	In stock	$ 1,490.00
100 mg	In stock	$ 1,970.00

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Purity: 100%

Purity: 99.71%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

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]

Synonyms	NSC-364432, SarCNU, Sarcosinamide, NSC 364432, NSC364432
Molecular Weight	222.63
Formula	C6H11ClN4O3
CAS No.	81965-43-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (224.59 mM)

References and Literature

1. Skalski V, et al. Mechanisms of resistance to (2-chloroethyl)-3-sarcosinamide-1-nitrosourea (SarCNU) in sensitive and resistant human glioma cells. Mol Pharmacol. 1990;38(3):299-305. 2. Noë AJ, et al. Transport of (2-chloroethyl)-3-sarcosinamide-1-nitrosourea in the human glioma cell line SK-MG-1 is mediated by an epinephrine-sensitive carrier system. Mol Pharmacol. 1993;44(1):204-209. 3. Marcantonio D, et al. 2-Chloroethyl-3-sarcosinamide-1-nitrosourea, a novel chloroethylnitrosourea analogue with enhanced antitumor activity against human glioma xenografts. Cancer Res. 1997;57(18):3895-3898. 4. Supko JG, et al. Plasma pharmacokinetics and bioavailability of 1-(2-chloroethyl)-3-sarcosinamide-1-nitrosourea after intravenous and oral administration to mice and dogs. Cancer Chemother Pharmacol. 2001;48(3):202-208. 5. Noë AJ, et al. Altered cytotoxicity of (2-chloroethyl)-3-sarcosinamide-1-nitrosourea in human glioma cell lines SK-MG-1 and SKI-1 correlates with differential transport kinetics. Cancer Res. 1994;54(6):1491-1496.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

Sarmustine 81965-43-7 NSC-364432 SarCNU Sarcosinamide NSC 364432 NSC364432 inhibitor inhibit

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