Temozolomide
Temozolomide, an alkylating agent, is a DNA damage inducer.
- 1. Fanchu Zeng, Zhijin Fan, et al. "Tumor Microenvironment Activated Photoacoustic-Fluorescence Bimodal Nanoprobe for Precise Chemo-immunotherapy and Immune Response Tracing of Glioblastoma." ACS Nano. 2023 Oct 24;17(20):19753-19766. PMID: 37812513
- 2. Schwartz, Hannah, et al. "In vitro Methods to Better Evaluate Drug Responses in Cancer." UMass Chan Medical School. September 8, 2022.
Physical Appearance | A solid |
Storage | Store at -20°C, sealed storage, away from moisture and light |
M.Wt | 194.15 |
Cas No. | 85622-93-1 |
Formula | C6H6N6O2 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥29.61 mg/mL in DMSO |
Chemical Name | 3-methyl-4-oxoimidazo [5,1-d] [1,2,3,5] tetrazine-8-carboxamide |
SDF | Download SDF |
Canonical SMILES | CN1C(=O)N2C=NC(=C2N=N1)C(=O)N |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment [1]: | |
Cell lines |
SK-LMS-1 leiomyosarcoma (MGMT-/p53+), Ewing sarcoma A-673 and GIST-T1 (both lines with MGMT+/p53- phenotype), and glioblastoma T98G (MGMT+/p53+) |
Preparation method |
The solubility of this compound in DMSO is >6.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
Reacting condition |
62.5, 125, 250 and 500 μM; 72 h |
Applications |
In SK-LMS-1 cells, Temozolomide inhibited proliferative activity of SK-LMS-1 cells. A-673 cells was most sensitive to temozolomide, the effect was time- and dose-dependent. Preincubation of Ewing sarcoma cells with O6-benzylguanine potentiated the cytotoxic effect of the alkylating agent and reduced viability of tumor cells. GIST-T1 cells were insensitive to temozolomide. |
Animal experiment [2]: | |
Animal models |
PARP1 wild‐type (WT) and PARP1 knock‐out (KO) mice |
Dosage form |
68 mg/kg; once daily for 5 days; orally administrated |
Application |
In PARP1 WT mice, temozolomide significantly lowered concentrations of NAD+ in the liver when compared with the control group (by 22%, p = 0.02). In the livers of PARP1 KO mice, there was also a statistically significant reduction in NAD+ in the temozolomide‐only group when compared with the control (by 22%, p = 0.03). |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Khusnutdinov RR1, Boichuk SV2. Mechanisms of Sensitivity of Soft Tissue Sarcoma Cells to Temozolomide. Bull Exp Biol Med. 2017 Jul 18. [2] Almeida GS1, Bawn CM1, Galler M1, et al. PARP inhibitor rucaparib induces changes in NAD levels in cells and liver tissues as assessed by MRS. NMR Biomed. 2017 May 22. |
Quality Control & MSDS
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