Rubitecan (RFS 2000)，喜树碱衍生物，是一种口服活性拓扑异构酶 I 抑制剂，具有广泛抗肿瘤活性，诱导蛋白质连接的 DNA 单链断裂，从而阻断分裂细胞中的 DNA 和 RNA 合成。
CAS：91421-42-0
分子式：C20H15N3O6
分子量：393.35
纯度：98%
存储：Store at -20°C

Background:

Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells[1][2][3]. Topoisomerase I[1]

Rubitecan (RFS 2000) inhibits U-CH1, U-CH2, and CCL4 cells with IC50s 0.32, 0.83, and 7.7 µM, respectively[4].

[1]. Burris HA 3rd, et al. Phase II trial of oral rubitecan in previously treated pancreatic cancer patients. Oncologist. 2005 Mar;10(3):183-90. [2]. Rubitecan: 9-NC, 9-Nitro-20(S)-camptothecin, 9-nitro-camptothecin, 9-nitrocamptothecin, RFS 2000, RFS2000. Drugs R D. 2004;5(5):305-11. [3]. Rubitecan [4]. Xia M, et al. Identification of repurposed small molecule drugs for chordoma therapy. Cancer Biol Ther. 2013 Jul;14(7):638-47.