TMZ(Temozolomide)

製品コードS1237 バッチS123708

印刷

化学情報

Chemical Structure 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) 20 mg/mL (103.01 mM)
Water (warmed with 50ºC water bath) 2.5 mg/mL (12.87 mM)
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 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。

 5.000mg/ml (25.75mM) Taking the 1 mL working solution as an example, add 50 μL of 100 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/

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

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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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