Temozolomide

Temozolomide is a prodrug form of the DNA alkylating agent MTIC (Cay-18863). It is converted to MTIC in a non-enzymatic manner under physiological conditions. Temozolomide is selectively cytotoxic to U87 and D54 glioblastoma cells, which do not express O6-methylguanine-DNA methyltransferase (MGMT), over MGMT-expressing T98G and U3054MG glioblastoma cells (IC50s = 51, 12, 660, and 370 µM, respectively). It increases survival in a Br23c glioblastoma orthotopic mouse xenograft model when administered at a dose of 15 mg/kg. Temozolomide, in combination with antibodies targeting CD47, decreases tumor volume and increases the number of tumor-infiltrating CD4+ and CD8+ T cells in a GL261 murine glioma model. Formulations containing temozolomide have been used in the treatment of glioblastoma multiforme (GBM) and refractory anaplastic astrocytoma.Formal Name: 3,4-dihydro-3-methyl-4-oxo-imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide. CAS Number: 85622-93-1. Synonyms: CCRG 81045, MB 39831, Methazolastone, NSC 362856, TMZ. Molecular Formula: C6H6N6O2. Formula Weight: 194.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 5 mg/ml, PBS (pH 7.2): 0.33 mg/ml. lambdamax: 209, 254, 327 nm. SMILES: CN1N=NC2=C(C(N)=O)N=CN2C1=O. InChi Code: InChI=1S/C6H6N6O2/c1-11-6(14)12-2-8-3(4(7)13)5(12)9-10-11/h2H,1H3,(H2,7,13). InChi Key: BPEGJWRSRHCHSN-UHFFFAOYSA-N.