Rigosertib (ON-01910 sodium salt) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM. Rigosertib (ON-01910) inhibited polo-like kinase1 (Plk1), induced apoptosis in CLL B cells without significant toxicity against T cells or normal B cells. Rigosertib also inhibits several multidrug resistant tumor cell lines, including MES-SA, MES-SA/DX5a, CEM, and CEM/C2a, with IC50 of 50-100 nM. Rigosertib also abrogates the pro-survival effect of follicular dendritic cells on CLL cells and reduces SDF-1-induced migration of leukemic cells. Rigosertib (200 mg/kg) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells in vivo.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL
Water 80 mg/mL
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.
Chapman CM, et al. Clin Cancer Res. 2012 Apr 1;18(7):1979-91. PMID: 22351695.
Phase I study of Rigosertib, an inhibitor of the phosphatidylinositol 3-kinase and Polo-like kinase 1 pathways, combined with gemcitabine in patients with solid tumors and pancreatic cancer.
Ma WW, et al. Clin Cancer Res. 2012 Apr 1;18(7):2048-55. PMID: 22338014.
|Related PLK Products|
HMN-214 is a procompound of HMN-176, which alters the cellular spatial orientation of Plk1.
TAK-960 is a novel, potent and selective Plk1 inhibitor with IC50 of 8 nM.
RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.
MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.
GW 843682X is a PLK inhibitor for PLK1 and PLK3 with IC50 of 2.2 nM and 9.1 nM, respectively.
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