Temozolomide

Description

Biological Activity

Protocol(Only for Reference)

Chemical Information

Cell Assay: [1]

Animal Study: [1]

References

貨號 Cat. No.: S1237
規格 Size: 10mM/1mLã€100mg
品牌 Brand: Selleckchem

Temozolomide

Catalog No.S12371 Product Citations

Temozolomide is a DNA damage inducer.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 80	In stock	0 1 2 3 4 5 6 7 8 9 10
25mg	USD 88	In stock	0 1 2 3 4 5 6 7 8 9 10
100mg	USD 214	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Cell lines	L-1210 and L-1210/BCNU cells
Concentrations	0 μM -100 μM
Incubation Time	l hours
Method	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.

Animal Models	DBA/2 mice with L-1210 and L-1210/BCNU cells
Dosages	40 mg/kg
Administration	Administered via i.v.
Solubility	1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL

Description

Temozolomide is a DNA damage inducer.

In vitro

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. In L-1210 but not in L-1210/BCNU methazolastone induces an arrest of cells in SL-G2-M phases. Methazolastone induces a similar amount of DNA ALS which is also repaired at a similar rate in L-1210 and L-1210/BCNU cell lines. Methazolastone induces a similar amount of DNA ALS which is also repaired at a similar rate in L-1210 and L-1210/BCNU cell lines. [1] 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. [2] Methazolastone induces in monocytes the DNA damage response pathways ATM-Chk2 and ATR-Chk1 resulting in p53 activation. [3] Chronic Methazolastone exposure results in acquired Methazolastone-resistance and elevates miR-21 expression. [4]Methazolastone treatment triggers endoplasmic reticula (ER) stress with increased expression of GADD153 and GRP78 proteins, and deceases pro-caspase 12 protein. Methazolastone induces autophagy through mitochondrial damage- and ER stress-dependent mechanisms to protect glioma cells. [5]

After 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. [1]

Methazolastone is a second-generation alkylating agent.

Download Temozolomide SDF

Molecular Weight (MW)	194.15
Formula	C6H6N6O2
CAS No.	85622-93-1

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	Methazolastone, Temodar, Temodal

Solubility (25°C) *	In vitro	DMSO	39 mg/mL (200 mM)
		Water	5 mg/mL (25 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	1% DMSO/30% polyethylene glycol/1% Tween 80,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.