TMZ(Temozolomide)

別名：NSC 362856,CCRG 81045,Methazolastone

製品コード：S1237 純度：99.99%

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。

CAS No. 85622-93-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
25mg	JPY 22000	国内在庫あり
100mg	JPY 41500	国内在庫あり
1g	JPY 101500	国内在庫あり
5g	JPY 295500	国内在庫なし(納期7~10日)
10g	JPY 445500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

DNA/RNA Synthesisシグナル伝達経路

DNA/RNA Synthesis阻害剤の選択性比較

阻害剤	Citation	AChR	mAChR	nAChR	AChE	muscarinic receptors	その他
(-)-Huperzine A (HupA)	1				++++
PNU-120596	8			+++
4-DAMP	0		++++
VU 0365114	0		++
Pseudocoptisine chloride	0				+
Pimethixene maleate	0		++++				5-HT2B,5-HT2A,Histamine H1 Receptor
Myosmine	0			++
Caulophylline (N-Methylcytisine)	0			+++			NF-κB,IKK,IκB
VU0119498	0		+
VU0238441	0		++
RHC 80267	0	+
NS 1738	0			++			<i>Xenopus laevis</i> oocyte α7 nAChR
VU0238429	0		++
Batefenterol	0		++++				hβ2-adrenoceptor
Nodakenin	0
Jatrorrhizine chloride	0
Imidafenacin	0		++++
Tropisetron	2			++++			5-HT3 receptor
Acotiamide	0
Isoimperatorin	0
Jatrorrhizine	0
Palmatine	1						BChE
Loganin	0				++		BChE,BACE1
Itopride hydrochloride	0				++		dopamine D2-receptor
Benzethonium Chloride	5			+++
Hyoscyamine	1	+++				+++
Adiphenine HCl	0			++
Otilonium Bromide	2		✔
Irsogladine	0	✔					PDE
(-)-Carvone	0				✔
Sofpironium bromide	0		✔
Nitrocaramiphen hydrochloride	0		✔
Vasicine (hydrochloride)	0				✔		BChE
W-84 Dibromide	0	✔
Picfeltarraenin IB	0				✔
Nodakenetin	0				✔		RLAR,PTP1B,α-glucosidase
α-Conotoxin GI	0			✔
BNC210	0			✔
Huperzine B	0				✔
Dehydroevodiamine hydrochloride	0				✔
Pentoxyverine Citrate	0		✔
Hexamethonium Dibromide	0	✔					Dopamine subtype 2 receptor
Catharanthine	0			✔

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
U251	Function Assay	15 μM	24 h	increases DNA-fragmentation in NPe6-PDT treated glioma cells	25262961
T98G	Function Assay	15 μM	24 h	increases DNA-fragmentation in NPe6-PDT treated glioma cells	25262961
U251	Growth Inhibition Assay	5/10/15 μM	24 h	induces cell death dose-dependently after concomitant-temozolomide with NPe6-PDT	25262961
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生物活性

製品説明

特性

Methazolastone is a second-generation alkylating agent.

Targets

DNA replication ^[1]
(L-1210, L-1210/BCNU cells)

In Vitro
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]
細胞実験	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.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	DR5 / c-FLIP / Survivin / XIAP pERK / ERK / p-p38 / p38		24436439
	Growth inhibition assay	Cell viability		25751281
	Immunofluorescence	Phalloidin / Phospho-H2A.X cleaved caspase-3		27375225

In Vivo
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]
動物実験	動物モデル	DBA/2 mice with L-1210 and L-1210/BCNU cells
	投与量	40 mg/kg
	投与経路	Administered via i.v.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05128734	Not yet recruiting	Breast Cancer Triple Negative	AHS Cancer Control Alberta	July 1 2024	Phase 2
NCT06161974	Not yet recruiting	High Grade Glioma\|Astrocytoma\|Astrocytoma Grade III\|Astrocytoma Grade IV\|Diffuse Intrinsic Pontine Glioma\|WHO Grade III Glioma\|WHO Grade IV Glioma\|Metastatic Brain Tumor\|Diffuse Midline Glioma H3 K27M-Mutant\|Thalamus Tumor\|Spinal Tumor\|IDH1 Mutation\|IDH1 R132\|IDH1 R132C\|IDH1 R132H\|IDH1 R132S\|IDH1 R132G\|IDH1 R132L\|Oligodendroglioma	Rigel Pharmaceuticals\|Nationwide Children''s Hospital	June 2024	Phase 2
NCT04967690	Not yet recruiting	Newly Diagnosed Glioblastoma	Double Bond Pharmaceutical AB	January 2024	Phase 1
NCT05698524	Recruiting	Recurrent High Grade Glioma\|Anaplastic Astrocytoma\|Anaplastic Oligodendroglioma\|Glioblastoma\|Gliosarcoma	University of Nebraska\|Xynomic Pharmaceuticals Inc.	June 26 2023	Phase 1
NCT04945148	Not yet recruiting	Glioblastoma IDH-wildtype	Hopital Foch\|National Cancer Institute France	May 2023	Phase 2

参考
[1] Catapano CV, et al. Cancer Res. 1987, 47(18), 4884-4889. [2] Sun S, et al. J Neurooncol. 2012. [3] Bauer M, et al. PLoS One. 2012, 7(6):e39956. [4] Wong ST, et al. Anticancer Res. 2012, 32(7), 2835-2841. [5] Lin CJ, et al. PLoS One. 2012, 7(6), e38706. [6] Gori JL, et al. Cancer Gene Ther. 2012. + 展開

参考

+ 展開

化学情報

分子量	194.15	化学式	C₆H₆N₆O₂
CAS No.	85622-93-1	SDF	Download TMZ(Temozolomide) SDFをダウンロードする
Smiles	CN1C(=O)N2C=NC(=C2N=N1)C(=O)N
保管	3 years-20°C （in the dark）powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3 years-20°C （in the dark）powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 39 mg/mL ( (200.87 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 7 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5%DMSO 1 30%PEG300 Click to order 2 65%ddH2O	2.0mg/ml (10.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 650 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5% DMSO 1 95% Corn oil	0.4mg/ml (2.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O	2.0mg/ml (10.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 Corn oil	2.0mg/ml (10.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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