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TEMOZOLOMIDE(TMZ NSC 362856)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TEMOZOLOMIDE(TMZ NSC 362856)图片
CAS NO:85622-93-1
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)194.15
FormulaC6H6N6O2
CAS No.85622-93-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 38 mg/mL (195.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)5% DMSO+30% PEG 300+ddH2O: 2 mg/mL
SynonymsCCRG81045, NSC362856; NSC 362856; CCRG 81045; NSC-362856; CCRG-81045; SCH-52365; SCH52365; SCH 52365; MB39831; MB-39831; MB 39831; RP46161; RP 46161; R-P46161; CCRG81045; TMZ. US trade names: Methazolastone; Temodar. Foreign brand name: Temodal
实验参考方法
In Vitro

In vitro activity: Methazolastone causes formation of DNA alkali-labile sites which are present in similar amounts and repaired at a similar rate in L-1210 and L-1210/BCNU cell lines. In L-1210 but not in L-1210/BCNU methazolastone induces an arrest of cells in SL-G2-M phases. Methazolastone sensitivity of both chemo-sensitive and resistant cells (D54-R and U87-R) is enhanced significantly under hyperoxia. Both Methazolastone and hyperoxia are associated with increased phosphorylation of ERK p44/42 MAPK (Erk1/2), but to a lesser extent in D54-R cells, suggesting that Erk1/2 activity may be involved in regulation of hyperoxia and Methazolastone-mediated cell death. Hyperoxia enhances Methazolastone toxicity in GBM cells by induction of apoptosis, possibly via MAPK-related pathways. Methazolastone induces in monocytes the DNA damage response pathways ATM-Chk2 and ATR-Chk1 resulting in p53 activation. Chronic Methazolastone exposure results in acquired Methazolastone-resistance and elevates miR-21 expression.


Cell Assay: L-1210 and L-1210/BCNU cells are seeded at 0.2 × 104 cells/mL and incubated for 24 hours. The cultures are treated with Methazolastone for l hours at 37oC, then washed twice in PBS by centrifugation and resuspended in fresh medium. Controls and treated samples are diluted in fresh medium 1:4 at 48 hours and 1:2 at 96 hours. Using these dilutions cell concentrations throughout the experiments are between 3 × 105 and 8 × 105/mL. Control growth is logarithmic in this range.

In VivoAfter a daily i.p. dose of 40 mg/kg for 5 consecutive days (days 1-5 after tumor transplant), methazolastone increases life-span by 86% in L-1210 and 22% in L-1210/BCNU. In L-1210/BCNU no effect is seen after 100 μM or 200 μM treatment; only 400 μM methazolastone produced an accumulation of cells in premitotic phase but much less than in L-1210. In L-1210/BCNU the maximum accumulation of cells in SL-G2-M is, after 48 hours-72 hours, approximately 30% as compared to 23% in untreated cells. Cells accumulates in SL-G2-M occurred too when L- 1210 leukemia-bearing mice are treated i.v. with methazola stone (40 mg/kg). No such effect is seen on L-1210/BCNU cells from mice given the same drug dose.
Animal modelDBA/2 mice with L-1210 and L-1210/BCNU cells
Formulation & DosageDissolved in 95% ethanol; 40 mg/kg; i.v. injection
ReferencesCancer Res. 1987 Sep 15;47(18):4884-9.