Tezacitabine (C09-1182-736)

Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue . Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair . Tezacitabine effectively induces cells apoptotic . Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatmentIn VitroTezacitabine (0.01-10 µM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment induces the G1 and S-phase leaky block of the cell cycle. Tezacitabine (0.01-10 µM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner. Tezacitabine has strong cytostatic and cytotoxic properties. Cytotoxic effect of Tezacitabine reveals not only as apoptosis, but also as a change in protein metabolism. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells Concentration: 0.01 µM, 0.1 µM, 1.0 µM, and 10 µM Incubation Time: 24 hours Result: Induced the G1 (at concentrations higher than 10 nM) and S-phase (at low concentration) leaky block of the cell cycle. Apoptosis AnalysisCell Line: CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells Concentration: 0.01 µM, 0.1 µM, 1.0 µM, and 10 µM Incubation Time: 24 hours Result: Induced apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner.In VivoTezacitabine (100 mg/kg; intraperitoneal injection; daily; female nude mice) treatment inhibits tumor growth in HCT 116 tumor xenografts. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female nude mice (7-9-week-old) injected with HCT 116 cellsDosage: 100 mg/kg Administration: Intraperitoneal injection; daily; 14 days Result: Inhibited tumor growth in HCT 116 tumor xenografts.Form:SolidIC50& Target:Ribonucleotide reductase. Specification: 0.99 Molecular Formula: C10H12FN3O4 Molecular Weight: 257.22 PubChem CID: 6435808 Isomeric SMILES: C1=CN(C(=O)N=C1N)[C@H]2/C(=C/F)/[C@@H]([C@H](O2)CO)O