SNS-314 Mesylate是一种ATP竞争性、选择性、强效Aurora kinase抑制剂,作用于Aurora A,Aurora B和Aurora C,IC50分别为9 nM,31 nM和3 nM。SNS-314对多种人癌细胞具有广泛的抑制增殖作用,IC50为1.8 nM-24 nM,并抑制组蛋白H3磷酸化(Ser 10)。在多种人移植瘤小鼠模型中,SNS-314也表现出抗肿瘤活性,抑制肿瘤生长,包括PC-3、H1299、A2780、MDA-MB-231和A375。
目前,SNS-314 Mesylate已进入临床Phase 1阶段。
【该产品仅用于科研实验,不能用于人体】
参考文献
[1] Oslob JD, et al. Discovery of a potent and selective aurora kinase inhibitor. Bioorg Med Chem Lett, 18(17): 4880-4884(2008).
[2] Arbitrario J P, et al. SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer chemotherapy and pharmacology, 65(4): 707-717(2010).
[3] VanderPorten EC, et al. The Aurora kinase inhibitor SNS-314 shows broad therapeutic potential with chemotherapeutics and synergy with microtubule-targeted agents in a colon carcinoma model. Mol Cancer Ther 8(4):930–939(2009).
粉末直接保存于-20 ºC,有效期2年。易溶于DMSO。建议分装后-20ºC避光保存,避免反复冻存,至少可存放6个月。