TMZ(Temozolomide)

製品コードS1237 バッチS123711

印刷

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 (warmed with 50ºC water bath)

39 mg/mL (200.87 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.000mg/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 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.400mg/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.

* <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	Temozolomide (TMZ) 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 it induces an arrest of cells in SL-G2-M phases.^[1] Its sensitivity of both chemo-sensitive and resistant cells (D54-R and U87-R) is enhanced significantly under hyperoxia. Both this compound 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 TMZ-mediated cell death. Hyperoxia enhances its toxicity in GBM cells by induction of apoptosis, possibly via MAPK-related pathways. ^[2] It induces in monocytes the DNA damage response pathways ATM-Chk2 and ATR-Chk1 resulting in p53 activation. ^[3] Chronic exposure results in acquired TMZ-resistance and elevates miR-21 expression. ^[4] Its treatment triggers endoplasmic reticula (ER) stress with increased expression of GADD153 and GRP78 proteins, and deceases pro-caspase 12 protein. This compound 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), TMZ (Temozolomide) 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 of this compound 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 it (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 TMZ (Temozolomide) for l hours at 37oC, then washed twice in PBS by centrifugation and resuspended in fresh medium. This compound is used in controls and treated samples, which 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

https://pubmed.ncbi.nlm.nih.gov/3621181/
https://pubmed.ncbi.nlm.nih.gov/22763762/
https://pubmed.ncbi.nlm.nih.gov/22768182/

https://pubmed.ncbi.nlm.nih.gov/22753745/
https://pubmed.ncbi.nlm.nih.gov/22745676/
https://pubmed.ncbi.nlm.nih.gov/22627392/

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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：

Cisplatin and temozolomide combinatorial treatment triggers hypermutability and immune surveillance in experimental cancer models [ Cancer Cell, 2025, S1535-6108(25)00223-5]	PubMed: 40513578
Proteogenomic characterization of non-functional pancreatic neuroendocrine tumors unravels clinically relevant subgroups [ Cancer Cell, 2025, 43(4):776-796.e14]	PubMed: 40185092
HR eye & MMR eye: one-day assessment of DNA repair-defective tumors eligible for targeted therapy [ Nat Commun, 2025, 16(1):4239]	PubMed: 40355434
Calnexin promotes glioblastoma progression by inducing protective mitophagy through the MEK/ERK/BNIP3 pathway [ Theranostics, 2025, 15(6):2624-2648]	PubMed: 39990231
Overexpression of miR-124 enhances the therapeutic benefit of TMZ treatment in the orthotopic GBM mice model by inhibition of DNA damage repair [ Cell Death Dis, 2025, 16(1):47]	PubMed: 39865088
Transketolase attenuates the chemotherapy sensitivity of glioma cells by modulating R-loop formation [ Cell Rep, 2025, 44(1):115142]	PubMed: 39792560
CDK12 regulates cellular metabolism to promote glioblastoma growth [ JCI Insight, 2025, 10(21)e190780]	PubMed: 40996961
EZH2 inhibition sensitizes MYC-high medulloblastoma cancers to PARP inhibition by regulating NUPR1-mediated DNA repair [ Oncogene, 2025, 44(6):391-405]	PubMed: 39562655
DNA methylation remodeling in temozolomide resistant recurrent glioblastoma: comparing epigenetic dynamics in vitro and in vivo [ J Transl Med, 2025, 23(1):779]	PubMed: 40640872
Siramesine induced cell death of glioblastoma through inactivating the STAT3-MGMT signaling pathway [ J Transl Med, 2025, 23(1):780]	PubMed: 40640878

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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