| CAS NO: | 24386-93-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 392.15 |
|---|---|
| Formula | C11H13IN4O4 |
| CAS No. | 24386-93-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 78 mg/mL (198.9 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| SMILES | NC1=C2C(N([C@H]3[C@H](O)[C@H](O)[C@@H](CO)O3)C=C2I)=NC=N1 |
| Synonyms | NSC 113939, 5-ITu; NSC113939; 5ITu; NSC-113939; 5 ITu; NSC 113939; 5 ITu |
| In Vitro | In vitro activity: 5-Iodotubercidin(Itu) is a genotoxic drug that activates the Atm-p53 pathway and has anti-tumor activity. Itu is unique compared to other nucleoside analogs in the way that it induces G2 arrest in a p53 -dependent manner. Moreover, at higher doses, Itu might activate p53-independent pathways, which may cooperate with p53 to kill cells and inhibit tumor growth. Incorporation of Itu metabolite into DNA causes DNA breaks, which triggers the DNA damage response. Itu might be a potential chemotherapeutic drug with distinct working mechanisms. Kinase Assay: 5-Iodotubercidin(NSC 113939; 5-ITu) is a potent adenosine kinase inhibitor (IC50 = 26 nM). Cell Assay: In various cells such as cancer cells, persisted AMPK activation could result in apoptosis [4]. In nude mice with colon carcinoma xenograft, Itu at a dose of 2.5 mg/kg resulted in rapid tumor regression compared with the control group. At the dose of 0.625 mg/kg, Itu still inhibited tumor growth, but p53-/- tumors were resistant to Itu at this lowered dose. |
|---|---|
| In Vivo | 5-Iodotubercidin is a potent inhibitor of adenosine kinase in the rat brain. 5-iodotubercidin has potent hypotensive, muscle relaxant, and hypothermic actions in mice, and that these effects could be blocked by theophylline, an adenosine receptor antagonist. 5-iodotubercidin (1 mg/kg, i.p.) administered prior to an ischemic episode, fails to provide a degree of cerebroprotection, assessed either by locomotor or histopathological indices Even though 5-iodotubercidin administration is known to enhance extracellular adenosine levels in brain slices |
| Animal model | Male Mongolian gerbils |
| Formulation & Dosage | Dissolved in saline; 1, 2.5 and 5 mg/kg; i.p. injection |
| References | Life Sci. 1993;53(6):497-502; PLoS One. 2013 May 7;8(5):e62527. |
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