TMZ(Temozolomide)

Catalog No.S1237 Batch:S123709

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Technical Data

Formula

C6H6N6O2
Molecular Weight 194.15 CAS No. 85622-93-1
Solubility (25°C)* In vitro DMSO 19 mg/mL (97.86 mM)
Water 3 mg/mL (15.45 mM)
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
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.
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Temozolomide (TMZ) is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. It is a DNA damage inducer in L-1210 and L-1210/BCNU cells. This compound induces apoptosis and exhibits antitumor activity.
Targets
DNA replication [1]
(L-1210, L-1210/BCNU cells)
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 this compound induces an arrest of cells in SL-G2-M phases. Its sensitivity of both chemo-sensitive and resistant cells (D54-R and U87-R) is enhanced significantly under hyperoxia. Both it 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. It induces in monocytes the DNA damage response pathways ATM-Chk2 and ATR-Chk1 resulting in p53 activation. Chronic exposure to this compound results in acquired TMZ-resistance and elevates miR-21 expression. Treatment with it triggers endoplasmic reticula (ER) stress with increased expression of GADD153 and GRP78 proteins, and deceases pro-caspase 12 protein. It induces autophagy through mitochondrial damage- and ER stress-dependent mechanisms to protect glioma cells.

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.

Features Methazolastone is a second-generation alkylating agent.

Protocol (from reference)

Cell Assay:

[1]
  • 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 TMZ (Temozolomide) 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 Study:

[1]
  • Animal Models

    DBA/2 mice with L-1210 and L-1210/BCNU cells

  • Dosages

    40 mg/kg

  • Administration

    Administered via i.v.

References

  • 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/

Customer Product Validation

C57BL/6 mice were implanted in the striatum with citrine-GL26-Cherry-HMGB1, which were stably transfected to express the YFP citrine and HMGB1 fused to red fluorescent protein cherry. Fourteen days later, they were treated with saline, Ad-TK+Ad-Flt3L, or Ad-TK+Ad-Flt3L+TMZ (temozolomide). Five days after treatment, the cellular location of cherry-HMGB1 in these cells was assessed by confocal microscopy. Arrows, tumor cells (green) with cytoplasmic HMGB1 (red).

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

D, Scramble (SCR), H82, H865, and H1836 cells were treated with AZD1775 (100 nmol/L) and temozolomide (1 μmol/L) for 24 hours; WEE1 KD cells were treated with just temozolomide (1 μmol/L) for 24 hours. The cells were lysed at 24 hours and subjected to Western blot analysis for phosphorylated WEE1 (pWEE1_S642), pCDC2_Y15 (WEE1 downstream effector), γH2AX (DNA damage marker), PH3 (mitotic marker), cleaved caspase-3 (apoptotic marker), and actin (loading control). E, SCR and WEE1 KD H82, H865, and H1836 cells were treated as described in D and subjected to Western blot analysis for DNA repair markers pATM_S1981, MRE11, RAD51, and E2F1. Actin was used as a loading control.

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

Talazoparib and temozolomide exhibit marked combinatorial efficacy in PDXs. A, Western blot against MGMT by near-infrared imaging in PDX models.

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

Data from [ , , J Control Release, 2018, 269:245-257 ]

Selleck's TMZ(Temozolomide) Has Been Cited by 267 Publications

CDK12/CDK13 inhibition disrupts transcriptional elongation and replication fork progression in glioblastoma [ EMBO Mol Med, 2026, 18(5):1592-1624.] PubMed: 41882177
MS4A4A promotes macrophages M2 polarization via NF-κB /JAK-STAT6 axis, resulting GBM malignant progression [ Oncogene, 2026, 45(24):2313-2326] PubMed: 42056558
Novel imidazotetrazine derivatives overcome temozolomide resistance in glioblastoma by inducing ferroptosis and apoptosis [ Cell Death Discov, 2026, 12(1):14] PubMed: 41513607
Impact of neuroendocrine neoplasm-specific systemic treatments on expression and function of CXCR4 in neuroendocrine tumor cells [ Sci Rep, 2026, 16(1):4339] PubMed: 41620429
Hyaluronan-Based Glioblastoma Tumor Constructs Maintain Patient Tumor Drug Responses and Genomic Parity [ Micromachines (Basel), 2026, 17(3)276] PubMed: 41900164
Epigenetic Activity of Cancer Therapy Drugs Revealed by HeLa TI Cell-Based Assay [ Epigenomes, 2026, 10(1)14] PubMed: 41892363
Single-cell protein activity analysis reveals aberrant myogenesis and IGF2-PI3K pathway dependencies in MYOD1-mutant rhabdomyosarcoma [ Sci Adv, 2026, 12(9):eaea6453] PubMed: 41758938
Heterogenous Model of Temozolomide Resistance in Glioblastoma Reveals Phenotypic Shifts in Drug Response and Migratory Potential [ Adv Nanobiomed Res, 2026, e202500244] PubMed: 41924544
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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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