Carmustine

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Chemical Structure| 154-93-8 同义名 : BCNU;bis-chloroethylnitrosourea;BCNU Becenum;FDA 0345;DTI 015;SRI 1720;SK 27702;Nitrumon;NCI-C04773;NSC 409962;Gliadel;BiCNU
CAS号 : 154-93-8
货号 : A448630
分子式 : C5H9Cl2N3O2
纯度 : 97%
分子量 : 214.05
MDL号 : MFCD00057706
存储条件:

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 35 mg/mL(163.51 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(467.18 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Carmustine is an antitumor chemotherapeutic agent, which works by akylating DNA and RNA. NAT (N-acetyltransferase) activity in glial tumor cell cytosols and intact tumor cells were decreased by carmustine in a dose-dependent manner. Carmustine (8, 80, and 800 µM) decreases N-acetyltransferase (NAT) activities for 2-aminofluorene (AF) and p-aminobenzoic acid (PABA) in rat glial tumor cytosol and intact cells. In rat glial tumor cells, the DNA-AF adduct increases, and carmustine decreases the formation of DNA-AF adduct[3]. Preincubation of cells with the glutathione reductase inhibitor, carmustine, led to elevated basal [Ca2+]i, yet the cells remained responsive to bradykinin[4]. Carmustine (≥25 µM) stimulates eryptosis at least partially by increasing cytosolic Ca²⁺ activity[5]. Carmustine (BCNU; 25 mg/kg, i.p.) causes higher levels of the rhe ratio of liver weight to body weight and plasma conjugated bilirubin, and lower biliary flow, oxidised glutation levels (GSSG) and reduced glutation (GSH)/GSSG values compared with control rats[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.67mL

0.93mL

0.47mL

23.36mL

4.67mL

2.34mL

46.72mL

9.34mL

4.67mL

参考文献

[1]Doishita S, Shimono T, et al. In vitro Study of Serial Changes to Carmustine Wafers (Gliadel) with MR Imaging and Computed Tomography. Magn Reson Med Sci. 2017 Sep 4.

[2]Lin SH, Kleinberg LR. Carmustine wafers: localized delivery of chemotherapeutic agents in CNS malignancies. Expert Rev Anticancer Ther. 2008 Mar;8(3):343-59.

[3]Hung CF. Effects of carmustine and lomustine on arylamine N-acetyltransferase activity and 2-aminofluorene-DNA adducts in rat glial tumor cells. Neurochem Res. 2000 Jun;25(6):845-51

[4]Elliott SJ, Schilling WP. Carmustine augments the effects of tert-butyl hydroperoxide on calcium signaling in cultured pulmonary artery endothelial cells. J Biol Chem. 1990 Jan 5;265(1):103-7

[5]Jilani K, Lang F. Carmustine-induced phosphatidylserine translocation in the erythrocyte membrane. Toxins (Basel). 2013 Apr 19;5(4):703-16

[6]Demir A, Özütemiz O, Yildiz C, Yüce G, Tekeşin O, Ilter T. The effect of trimetazidine on intrahepatic cholestasis caused by carmustine in rats. Hepatol Res. 2001 May 1;20(1):133-143