| Description | Fiacitabine (NSC-382097) is a selective inhibitor of DNA replication of the herpes simplex virus(HSV) (IC50: 2.5 nM and 12.6 nM for HSV1 and HSV2, respectively). |
| In vitro | FIAC在浓度上远低于阿拉伯核苷酸胞嘧啶、碘脱氧尿苷和阿拉伯核苷酸腺苷时展现出活性。其对单纯疱疹病毒1型的活性轻微高于阿昔洛韦，对正常细胞的毒性也略高。对于野生型单纯疱疹病毒1型的复制，FIAC的活性约为缺失病毒特定胸苷激酶表达的突变株的8000倍。在0.0025至0.0126 microM的浓度下，HSV FIAC对单纯疱疹病毒1型和2型的各种株系的复制抑制率达到90%。通过使用吉姆萨染色法排除试验，确定在Noman Vero、WI-38和NC-37细胞增殖中的细胞毒性极小，4天测定的50%抑制剂浓度为4至10 microM [2]。 |
| Target activity | HSV2:12.6 nM, HSV1:2.5 nM |
| Synonyms | 非西他滨, FOAC, FIAC, NSC 382097 |
| molecular weight | 371.1 |
| Molecular formula | C9H11FIN3O4 |
| CAS | 69123-90-6 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 35 mg/mL (94.31 mM) |
| References | 1. Allaudeen HS, et al. Selective inhibition of DNA replication in herpes simplex virus infected cells by 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)-5-iodocytosine. J Biol Chem. 1982 Oct 25;257(20):11879-82. 2. Lopez C, et al. 2'-fluoro-5-iodo-aracytosine, a potent and selective anti-herpesvirus agent. Antimicrob Agents Chemother. 1980 May;17(5):803-6. |