ON-01910 是一种非 ATP 竞争性 PLK1 抑制剂（IC50 为 9 nM，在无细胞试验中）。它对 PLK2 的选择性高出 30 倍，对 PLK3 没有活性。 Rigosertib 抑制 PI3K/Akt 通路并激活氧化应激信号。 Rigosertib 可诱导多种癌细胞凋亡。它是一种合成的苄基苯乙烯基砜类似物，具有潜在的抗肿瘤活性。

ON-01910 is a non-ATP-competitive PLK1 inhibitor(IC50 of 9 nM, in a cell-free assay). It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells.It is a synthetic benzyl styryl sulfone analogue with potential antineoplastic activity.

ON01910, a small molecule inhibitor of Plk1 activity, which induces mitotic arrest of tumor cells characterized by spindle abnormalities leading to their apoptosis.?This compound was not ATP-competitive, but competed for the substrate binding site of the enzyme[1].

In vivo, this compound did not exhibit hematotoxicity, liver damage, or neurotoxicity, and was a potent inhibitor of tumor growth in a variety of xenograft nude mouse models.?ON01910 showed strong synergy with several chemotherapeutic agents, often inducing complete regression of tumors[1].

1225497-78-8

C21H24NNaO8S

473.47

N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐

DMSO:94 mg/mL (198.53 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years