TMZ(Temozolomide)

製品コードS1237 バッチS123707

化学情報

	Synonyms	NSC 362856,CCRG 81045,Methazolastone	Storage (From the date of receipt)	3 years-20°C （in the dark）powder
	化学式	C₆H₆N₆O₂
	分子量	194.15	CAS No.	85622-93-1
Solubility (25°C)*	体外	DMSO	20 mg/mL warmed with 50ºC water bath (103.01 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	テモゾロミド (Temozolomide (NSC 362856,TMZ,CCRG 81045,Methazolastone)) はDNA 環上の窒素原子と環外酸素を修飾することが可能な単官能性 SN1 アルキル化剤であり、中間体である MTIC を経て、活性代謝産物であるメチルジアゾニウムカチオン (methyl diazoniumcation) に分解されると、生理学的 pH において DNA にメチル基を転移します。テモゾロミドはアポトーシス (apoptosis) を誘発し、抗がん活性を呈します。L-1210 細胞および L-1210/BCNU 細胞における DNA 損傷誘導剤です。
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 cell lines. In L-1210 but not in L-1210/BCNU methazolastone induces an arrest of cells in SL-G2-M phases.^[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]
in vivo	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]
特徴	Methazolastone is a second-generation alkylating agent.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	L-1210 and L-1210/BCNU cells
	濃度	0 μM -100 μM
	反応時間	l hours
	実験の流れ	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.
動物実験	動物モデル	DBA/2 mice with L-1210 and L-1210/BCNU cells
	投薬量	40 mg/kg
	投与方法	Administered via i.v.

参考

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カスタマーフィードバック

: Data from [Data independently produced by Clin Cancer Res, 2014, 20(6), 1555-65]

: Data from [Data independently produced by , , Clin Cancer Res, 2017, 23(20):6239-6253]

: Data from [Data independently produced by , , Clin Cancer Res, 2017, 23(2):523-535]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Integration of 3D bioprinting and multi-algorithm machine learning identified glioma susceptibilities and microenvironment characteristics [ Cell Discov, 2024, 10(1):39]	PubMed: 38594259
GINS2 regulates temozolomide chemosensitivity via the EGR1/ECT2 axis in gliomas [ Cell Death Dis, 2024, 15(3):205]	PubMed: 38467631
Patient derived tumoroids of high grade neuroendocrine neoplasms for more personalized therapies [ NPJ Precis Oncol, 2024, 8(1):59]	PubMed: 38429350
The combination therapy using tyrosine kinase receptors inhibitors and repurposed drugs to target patient-derived glioblastoma stem cells [ Biomed Pharmacother, 2024, 176:116892]	PubMed: 38876048
A Novel Approach for Glioblastoma Treatment by Combining Apoptosis Inducers (TMZ, MTX, and Cytarabine) with E.V.A. (Eltanexor, Venetoclax, and A1210477) Inhibiting XPO1, Bcl-2, and Mcl-1 [ Cells, 2024, 13(7)632]	PubMed: 38607071
3D-printed implants loaded with acriflavine for glioblastoma treatment [ Int J Pharm, 2024, 665:124710]	PubMed: 39277153
Daurisoline suppress glioma progression by inhibiting autophagy through PI3K/AKT/mTOR pathway and increases TMZ sensitivity [ Biochem Pharmacol, 2024, 223:116113]	PubMed: 38460907
Establishment of tumor microenvironment-preserving organoid model from patients with intracranial meningioma [ Cancer Cell Int, 2024, 24(1):36]	PubMed: 38238738
Temozolomide and the PARP Inhibitor Niraparib Enhance Expression of Natural Killer Group 2D Ligand ULBP1 and Gamma-Delta T Cell Cytotoxicity in Glioblastoma [ Cancers (Basel), 2024, 16(16)2852]	PubMed: 39199623
p53/E2F7 axis promotes temozolomide chemoresistance in glioblastoma multiforme [ BMC Cancer, 2024, 24(1):317]	PubMed: 38454344

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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