ON-01910

ON-01910CAS号: 1225497-78-8分子式: C21H24NNaO8S分子量: 473.47描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
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.
纯度
97%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:94 mg/mL (198.53 mM)
生物活性
靶点
Flt1:42 nM(Cell-free assay), PDGFR:18 nM(Cell-free assay), Src:55 nM(Cell-free assay), Bcr-Abl:32 nM(Cell-free assay), PLK1:9 nM(Cell-free assay)
In vitro(体外研究)
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(体内研究)
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].