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Temozolomide

Catalog No. T1178 CAS 85622-93-1

Synonyms: NSC 362856, TZM, CCRG 81045, TMZ

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy.

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Temozolomide, CAS 85622-93-1

Pack Size	Availability	Price/USD
10 mg	In stock	$ 42.00
25 mg	In stock	$ 68.00
50 mg	In stock	$ 82.00
100 mg	In stock	$ 97.00
200 mg	In stock	$ 129.00
500 mg	In stock	$ 169.00
1 g	In stock	$ 249.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 99.87%

Purity: 98.43%

Purity: 98%

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Description	Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy.
In vitro	METHODS: Melanoma cells SK-mel-28, MM200, IgR3, Mel-FH were treated with Temozolomide (0-500 μM) for 72 h. Cell viability was examined using MTT. RESULTS: The p53 status and MGMT expression levels were correlated with the sensitivity of Temozolomide. MM200 and IgR3 (expressing wild-type p53 and low MGMT levels) showed comparable sensitivity to Temozolomide, with IC50 values of 23 and 22 μM, respectively, whereas SK mel-28 and Mel-FH (mutant-type p53 and high MGMT level) were resistant with IC50 values >256 and >247 μM. [1] METHODS: Melanoma cells MM200 and IgR3 were treated with Temozolomide (100 μM) for 24-72 h. The cell cycle was examined by Flow Cytometry. RESULTS: Temozolomide induced G2/M cell cycle arrest in MM200 and IgR3 cells. [1] METHODS: Human glioma cells U118 were treated with Temozolomide (250-500 μM) for 3-48 h. The m5C level in DNA was measured. RESULTS: The response of U118 cells to Temozolomide depends on the concentration and time of the reaction. The amount of m5C in DNA increased significantly within a short period of time after Temozolomide treatment. m5C(R) reached the highest level after 24 h of treatment with 500 μM Temozolomide. [2]
In vivo	METHODS: To assay antitumor activity in vivo, Temozolomide (68 mg/kg by gavage) and AG-014699 (1 mg/kg by intraperitoneal injection) were administered intraperitoneally to CD1 nu/nu mice harboring medulloblastomas D425Med, D283Med, or D384Med once daily for five days. RESULTS: AG-014699 enhanced the efficacy of Temozolomide in an in vivo model of medulloblastoma. [3] METHODS: To assay antitumor activity in vivo, Temozolomide (0.9 mg/kg orally once daily) and Aldox (16 mg/kg intravenously once weekly) were administered to Foxn1 nude mice bearing human glioblastoma U87MG once daily for five weeks. RESULTS: Combined treatment with Temozolomide and AldoxAldo induced significant tumor volume suppression and increased survival. [4]
Cell Research	Cell lines exposed to TMZ (with or without 5-Aza or O6-BG pre-treatment) were grown in 24-well plates under standard culture conditions for 6 days. Cytotoxicity was determined using the sulphorhodamine-B (SRB) method. Briefly, the cells were fixed with 10% trichloroacetic acid for 20 min at 4°C then washed three times with water. After 24 hours, cells were stained for 30 min at room temperature with 0.4% SRB dissolved in 1% acetic acid and then washed three times with 1% acetic acid. The plates were air-dried and the dye solubilized with 300 ml/well of 10 mM Tris base (pH 10.5) for 10 min on a shaker. The optical density of each well was measured spectrophotometrically using a Titertek multiscan colorimeter at 492 nm [2].
Animal Research	TZM was dissolved in dimethyl-sulfoxide (40 mg/mL), diluted in saline (5 mg/mL), and administered intraperitoneally on day 2 after tumor injection at 100 mg/kg or 200 mg/kg, doses commonly used for in vivo preclinical studies.15-17 Because cytotoxicity induced by TZM and PARP inhibitors can be improved by fractionated modality of treatment,9 in selected groups a total dose of 200 mg/kg TZM was divided in 2 doses of 100 mg/kg given on days 2 and 3. NU1025 was dissolved in polyethylene glycol-400 (40% in saline) and was injected intracranially at the maximal deliverable dose (1 mg/mouse, 0.03 mL) or, in selected groups, intraperitoneally (0.3 mL) on day 2 after tumor challenge, 1 hour before TZM administration. Control mice were injected with drug vehicles [4].

Synonyms	NSC 362856, TZM, CCRG 81045, TMZ
Molecular Weight	194.15
Formula	C6H6N6O2
CAS No.	85622-93-1

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

PBS: 5 mg/mL (25.75 mM), Sonification is recommended

DMSO: 28.83mg/ml (200 mM)

References and Literature

1. Mhaidat NM, et al. Temozolomide induces senescence but not apoptosis in human melanoma cells. Br J Cancer. 2007 Nov 5;97(9):1225-33. 2. Barciszewska AM, et al. A New Epigenetic Mechanism of Temozolomide Action in Glioma Cells. PLoS One. 2015 Aug 26;10(8):e0136669. 3. Daniel RA, et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Br J Cancer. 2010 Nov 9;103(10):1588-96. 4. Da Ros M, et al. Aldoxorubicin and Temozolomide combination in a xenograft mice model of human glioblastoma. Oncotarget. 2018 Oct 9;9(79):34935-34944. 5. Daniel RA, et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. 6. Zhang B, Xu C, Liu J, et al. Nidogen-1 expression is associated with overall survival and temozolomide sensitivity in low-grade glioma patients[J]. Aging (Albany NY). 2021, 13(6): 9085. 7. Herbener V J, Burster T, Goreth A, et al. Considering the Experimental use of Temozolomide in Glioblastoma Research[J]. Biomedicines. 2020, 8(6): 151.

Citations

1. Wang Y, Wang X, Wang K, et al.Chronic stress accelerates glioblastoma progression via DRD2/ERK/β-catenin axis and Dopamine/ERK/TH positive feedback loop.Journal of Experimental & Clinical Cancer Research.2023, 42(1): 1-17. 2. Liu X, Guo C, Leng T, et al.Differential regulation of H3K9/H3K14 acetylation by small molecules drives neuron-fate-induction of glioma cell.Cell Death & Disease.2023, 14(2): 142. 3. Liu X, Guo Q, Gao G, et al.Exosome-transmitted circCABIN1 promotes temozolomide resistance in glioblastoma via sustaining ErbB downstream signaling.Journal of Nanobiotechnology.2023, 21(1): 1-25. 4. Chen Y, Guo Y, Li S, et al.Remdesivir inhibits the progression of glioblastoma by enhancing endoplasmic reticulum stress.Biomedicine & Pharmacotherapy.2023, 157: 114037. 5. Dong J, Peng Y, Zhong M, et al.Implication of lncRNA ZBED3-AS1 downregulation in acquired resistance to Temozolomide and glycolysis in glioblastoma.European Journal of Pharmacology.2022: 175444. 6. Tong S, Hong Y, Xu Y, et al.TFR2 regulates ferroptosis and enhances temozolomide chemo-sensitization in gliomas.Experimental Cell Research.2023: 113474. 7. Jiao W, Zhu S, Shao J, et al. ZSTK474 Sensitizes Glioblastoma to Temozolomide by Blocking Homologous Recombination Repair. BioMed Research International. 2022 8. Li J, Sun Y, Sun X, et al. AEG-1 silencing attenuates M2-polarization of glioma-associated microglia/macrophages and sensitizes glioma cells to temozolomide. Scientific reports. 2021, 11(1): 1-12. 9. Wang Y, Wang X, Wang X, et al. Imipramine impedes glioma progression by inhibiting YAP as a Hippo pathway independent manner and synergizes with temozolomide. Journal of Cellular and Molecular Medicine. 2021 10. Zhang B, Xu C, Liu J, et al. Nidogen-1 expression is associated with overall survival and temozolomide sensitivity in low-grade glioma patients. Aging (Albany NY). 2021 Mar 18;13(6):9085-9107. doi: 10.18632/aging.202789. Epub 2021 Mar 18.

11. Herbener V J, Burster T, Goreth A, et al. Considering the Experimental use of Temozolomide in Glioblastoma Research. Biomedicines. 2020, 8(6): 151 12. Li F, Chen S, Yu J, et al. Interplay of m6A and histone modifications contributes to temozolomide resistance in glioblastoma. Clinical and Translational Medicine. 2021, 11(9): e553 13. Zhang M, Ding Y, Gao M, et al.Discovery of Novel N-(Anthracen-9-ylmethyl) Benzamide Derivatives as ZNF207 Inhibitors Promising in Treating Glioma.Journal of Medicinal Chemistry.2024

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This product is contained In the following compound libraries：

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Keywords

Temozolomide 85622-93-1 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA Alkylator/Crosslinker DNA/RNA Synthesis NSC 362856 Inhibitor inhibit CCRG-81045 NSC362856 NSC-362856 TZM CCRG81045 CCRG 81045 TMZ inhibitor

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