ON-01910 sodium salt又称为Rigosertib、Estybon，是一种强效的、非ATP竞争性PLK1抑制剂（IC50=9 nM）。除PLK1，ON-01910还抑制多种蛋白激酶，如PLK2、PDGFR和CDK1等。ON-01910抑制多种癌细胞增殖，并诱导细胞周期阻滞在G2/M期，诱导多种肿瘤细胞凋亡，并抑制耐药性癌细胞生长。在体内，ON-01910也表现出明显的抗肿瘤效果，与化疗药物协同使用有效抑制体内肿瘤生长。

目前，ON-01910已用于临床Phase 3阶段。

【该产品仅用于科研实验，不能用于人体】

参考文献

[1] Gumireddy K, et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell 7(3): 275-286 (2005).

[2] Chapman CM, et al. ON 01910.Na is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Clinical Cancer Research 18(7): 1979-1991 (2012).

[3] Oussenko IA, et al. Effect of ON 01910.Na, an anticancer mitotic inhibitor, on cell-cycle progression correlates with RanGAP1 hyperphosphorylation. Cancer Research 71(14): 4968-4976 (2011).

[4] Chang KC, et al. Ran GTPase-activating protein 1 is a therapeutic target in diffuse large B-cell lymphoma. PLoS One 8(11): 1-12 (2013).

[5] Chun AW, et al. Preclinical pharmacokinetics and in vitro activity of ON 01910.Na, a novel anti-cancer agent. Cancer Chemother Pharmacol. 65(1): 177-186 (2009).

[6] Xu F, et al. Rigosertib as a selective anti-tumor agent can ameliorate multiple dysregulated signaling transduction pathways in high-grade myelodysplastic syndrome. Scientific Reports 7310 (2014).

冰袋运输。粉末直接保存于-20 ºC，有效期2年。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。