Temozolomide (NSC 362856, CCRG 81045) is a DNA methylating agent used for the treatment of Grade IV astrocytoma. Temozolomide exhibits schedule-dependent antineoplastic activity by interfering with DNA replication. Temozolomide displays antitumor activity against a board spectrum of tumors, including leukemias, lymphomas and solid tumors (IC50 = 5.0 μM for cytotoxicity against mouse TLX5 lymphoma cells). Temozolomide induces G2/M arrest and apoptosis through adduction of a methyl group to O6 position of guanine in genomic DNA and functional inactivation of DNA repair protein O(6)-alkylguanine DNA alkyltransferase (AGT) in base excision repair (BER) pathway. Temozolomide treatment triggered ER stress with increased expression of GADD153 and GRP78 proteins, and deceased pro-caspase 12 protein. Temozolomide is currently in a phase II clinical trial in the treatment of melanoma.
Sci Adv. 2022 May 13;8(19):eabn1229.
Translesion DNA synthesis mediates acquired resistance to olaparib plus temozolomide in small cell lung cancer
Temozolomide (TMZ) purchased from AbMole
Biochem Biophys Res Commun. 2021 Sep 10;569:1-9.
Rapid tumor recurrence in a novel murine GBM surgical model is associated with Akt/PD-L1/vimentin signaling
Temozolomide (TMZ) purchased from AbMole
bioRxiv. 2020 Oct.
Connexin 43 confers chemoresistance through activating PI3K
Temozolomide (TMZ) purchased from AbMole
Biomedicines. 2020 Jun 4;8(6):151.
Considering the Experimental use of Temozolomide in Glioblastoma Research
Temozolomide (TMZ) purchased from AbMole
Cancer Lett. 2020 Jun 1;479:1-12.
Exosome-mediated Transfer of circRNA CircNFIX Enhances Temozolomide Resistance in Glioma
Temozolomide (TMZ) purchased from AbMole
Cell. 2019 Jun 13;177(7):1903-1914.e14.
Visualizing Engrafted Human Cancer and Therapy Responses in Immunodeficient Zebrafish.
Temozolomide (TMZ) purchased from AbMole
J Clin Transl Sci. 2018 Nov 21;Vol2, Supplement S1, pp.11-12.
2036 Extracellular matrix as a novel approach to glioma therapy
Temozolomide (TMZ) purchased from AbMole
Cell Death Dis. 2018 Feb 12;9(2):213.
Autophagy mediates glucose starvationinduced glioblastoma cell quiescence and chemoresistance through coordinating cell metabolism, cell cycle, and survival
Temozolomide (TMZ) purchased from AbMole
Cancer Lett. 2016 Aug 28;379(1):134-42.
HDAC6 promotes cell proliferation and confers resistance to temozolomide in glioblastoma
Temozolomide (TMZ) purchased from AbMole
Cell Experiment | |
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Cell lines | A2058, A375, M238 and M249 cell lines |
Preparation method | Colony formation assay Depending on the cell line (and plating efficiency), 200–1000 cells were seeded into each well of a 6-well plate and treated as described in detail previously. In the case of primary melanoma cells, 1000 cells were seeded and let grow for 24 days in the presence or absence of drug treatment; because only small colonies formed, the stained colonies were counted under the microscope.Survival of melanoma cells after drug treatment. Five different melanoma cell lines (as indicated), as well as a culture of primary melanoma tissue cells (labeled ‘primary’) were exposed to increasing concentrations of TMZ (diamonds) or NEO212 (circles) for 48 hours, and long-term survival was determined via colony formation assay (CFA). |
Concentrations | 0, 25, 50, 75, 100µM |
Incubation time | 48 h |
Animal Experiment | |
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Animal models | A375 cells subcutaneous tumor growth model |
Formulation | 45% glycerol, 45% ethanol, 10% DMSO |
Dosages | 50 mg/kg |
Administration | subcutaneous injection |
Molecular Weight | 194.15 |
Formula | C6H6N6O2 |
CAS Number | 85622-93-1 |
Solubility (25°C) | DMSO 18 mg/mL |
Storage | -20°C, protect from light, sealed |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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