| Description | Diaziquone (NSC-182986) is a water-soluble synthetic azacyclic benzoquinone that enhances penetration of the blood-brain barrier, has antitumor activity, and is used in the treatment of extreme renal failure. |
| In vitro | Diaziquone（5000 ng/mL）与延长的造血功能抑制和罕见的骨髓坏死相关，但外骨髓毒性较轻。一小时和三小时处理对血液造血细胞与骨髓基质细胞的细胞毒性较小。六小时处理后，骨髓中的CFU-Mix、BFU-E和CFU-GM被耗尽，但在LTMCs中产生CFU-GM，表明从存活的前CFU-Mix细胞群中持续有CFU-GM输入。使用Diaziquone（150 ng/mL；3至7天）处理，从暴露于LTMCs中CFU-GM的缺失可推断后者被消除。 |
| In vivo | Diaziquone（每日0.1 mg；注射；4天），通过Vanicream、Plastibase或DMSO局部应用，分别在第20天抑制了肿瘤生长66%、86%和43%，并且以每日0.5 mg剂量治愈了动物的皮肤肿瘤。通过腹腔注射Diaziquone，每日0.5 mg，连续4天对大鼠是致命的，在0.1 mg/day剂量下，第20天抑制肿瘤生长93%。在注射肿瘤细胞12天后开始治疗，Diaziquone以每日0.1 mg，连续4天的剂量局部应用于Plastibase中，成功治愈了晚期肿瘤的大鼠。单次0.64-mg [ring-14C]diaziquone通过DMSO局部应用后，在5小时内血浆放射性时间曲线下面积仅为相同剂量的[ring-14C]diaziquone腹腔注射在无肿瘤大鼠中的0.01%。与腹腔注射同剂量的diaziquone相比，局部应用diaziquone后的WBC计数下降率，在Vanicream中为62%，在Plastibase中为81%，在DMSO中为33%。局部应用的Diaziquone对大鼠和家猪的正常皮肤无毒性。据此得出结论，Diaziquone的局部应用相较于系统性治疗，对转移性皮肤癌具有治疗优势。 |
| Synonyms | NSC 182986 |
| molecular weight | 364.35 |
| Molecular formula | C16H20N4O6 |
| CAS | 57998-68-2 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (123.51 mM) |
| References | 1. Schold SC Jr, et al. Treatment of human glioma and medulloblastoma tumor lines in athymic mice with diaziquone and diaziquone-based drug combinations. Cancer Res. 1984;44(6):2352-2357. 2. Moore DJ, et al. Topical chemotherapy of intradermal Walker 256 carcinosarcoma with diaziquone and doxorubicin in the rat. Cancer Res. 1985;45(11 Pt 1):5466-5472. 3. Lee EJ, et al. Diaziquone given as a continuous infusion is an active agent for relapsed adult acute nonlymphocytic leukemia. Blood. 1986;67(1):182-187. 4. Kushner BH, et al. Myeloablation with diaziquone: in vitro assessment. Blood. 1987;69(6):1747-1752. 5. Gutierrez PL, et al. Free radicals in quinone containing antitumor agents. The nature of the diaziquone (3,6,-diaziridinyl-2,5-bis(carboethoxyamino)-1,4-benzoquinone) free radical. Biochim Biophys Acta. 1983;758(1):37-41. 6. White L. Responsiveness of retinoblastoma to local diaziquone. Studies in a xenograft model. Invest Ophthalmol Vis Sci. 1990;31(5):787-791. |