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) treatment In Vitro Tezacitabine (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 Vivo Tezacitabine (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:Solid IC50& Target:Ribonucleotide reductase
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Tezacitabine
CAS number：130306-02-4 molecular formula：C10H12FN3O4
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| Chinese alias | 替扎他滨 | ||
| English alias | DB06433 | SCHEMBL18725 | KW-2331 | TEZACITABINE ANHYDROUS | 4-amino-1-[(2R,3E,4S,5R)-3-(fluoromethylidene)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one | MS-23621 | Tezacitabine, anhydrous [INN] | Tezacitabine, anhydrous | 2'-Deoxy-2'-(fluoromet | ||
| CAS number | 130306-02-4 | molecular formula | C10H12FN3O4 |
| molecular weight | 257.22 g/mol | Exact mass | ≥99% |
| PSA | 108.000 Ų | logp | -2.300 |
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