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KI1307Carmustine25 mg$114

Chemical Characteristic

Product NameCarmustine
SynonymsBCNU
CAS No.154-93-8
Molecular Weight 214.05
FormulaC5H9Cl2N3O2
Chemical NameBis(2-chloroethyl)nitrosourea; N,N-Bis (2-chloroethyl)-N-nitrosourea
SmilesN(C(=O)NCCCl)(N=O)CCCl
Chemical Structure

Biological activities

Carmustine is an alkylating agent in chemotherapy used in the treatment of several types of brain cancer (including glioma, glioblastoma multiforme, medulloblastoma and astrocytoma), multiple myeloma and lymphoma (Hodgkin's and non-Hodgkin). Carmustine is able to form interstrand crosslinks in DNA, which prevents DNA replication and DNA transcription. In vitro, carmustine inhibits [3H]thymidine incorporation into DNA with IC50 values of 71 and 57 µM in MCF-7 and MDA-MB-231cells, respectively.[1] The IC50 values of carmustine after 48 hours incubation to brain tumor cell lines GBM8401 and GBM8901 are 55.6 and 56.5 µg/mL, respectively.[2] In vitro, carmustine inhibits C6 glioma cell growth in a dose-dependent manner. In vivo, carmustine causes a dose-dependent inhibition of tumor growth rate in C6 glioma homografts with ID50 of 8.7 mg/kg.[3] Carmustine treatment (10 mg/kg) can potentially result in immediate increases in 9L gliosarcoma tumor oxygenation in rat.[4] In vivo, carmustine (35 mg/kg) also causes tumour growth delay of B16 melanoma and of human melanoma xenografts in immune-deprived mice. The combination of TNF with carmustine (35 mg/kg) makes a more significant growth delay in B16 melanoma compared with carmustine (35 mg/kg) alone.[5]

Protocols

In vivo: Carmustine is dissolved in 4% ethanol-saline.[4]

References

[1] Bielawski K, et al. Proline-linked nitrosoureas as prolidase-convertible prodrugs in human breast cancer cells. Pharmacol Rep. 2008, 60(2): 171-182.
[2] Tsai NM, et al. The antitumor effects of Angelica sinensis on malignant brain tumors in vitro and in vivo. Clin Cancer Res. 2005, 11(9): 3475-3484.
[3] Soma MR, et al. In vivo enhanced antitumor activity of carmustine [N,N'-bis(2-chloroethyl)-N-nitrosourea] by simvastatin. Cancer Res. 1995, 55(3): 597-602.
[4] Steen RG, et al. In vivo measurement of tumor blood oxygenation by near-infrared spectroscopy: immediate effects of pentobarbital overdose or carmustine treatment. J Neurooncol. 1994, 22(3): 209-220.
[5] Jones AL, et al. Enhanced anti-tumour activity of carmustine (BCNU) with tumour necrosis factor in vitro and in vivo. Br J Cancer. 1990, 62(5): 776-780.

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