administration of OTS964 causes some hematopoietic toxicity, this is a transient effect. The spontaneous recovery from leukocytopenia is occured and the anticancer effectiveness of the oral drug is similar to that of the liposomal formulation, oral administration of the drug may prove to be more ...
(72 nM), Daudi (25 nM), UM-UC-3 (32 nM), HCT-116 (33 nM),MKN1 (38 nM), MKN45 (39 nM), HepG2 (19 nM), MIAPaca-2 (30 nM), and 22Rv1 (50 nM)], whereas its growth inhibitory effect against TOPK-negative HT29 cancer cells is significantly weaker, with IC50 of 290nM...
Marcel B. Ballygrid.248762.d0000 0001 0702 3000Experimental TherapeuticsBC Cancer Agency, Vancouver Research Centre 675 W 10th Avenue (5th floor) V5Z 1L3 Vancouver BC CanadaSpringer USDrug Delivery and Translational Research
OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts. Targets TOPK (Cell-free assay); CDK11B (Cell-free assay) 28 nM; 40 nM(Kd) In vitro OTS964 inhibits the growth of TOPK-positive cells with low IC50 values [A549 (31...
this inhibitor causes a cytokinesis defect and the subsequent apoptosis of cancer cells in vitro as well as in xenograft models of human lung cancer. Although administration of the free compound induced hematopoietic adverse reactions (leukocytopenia associated with thrombocytosis), the drug delivered in...
Molecular imagingGlioblastomaTOPKPETOTS964Lymphokine-activated killer T cell-originated protein kinase (TOPK) is a fairly new cancer biomarker with great potential for clinical applications. The labeling of a TOPK inhibitor with F-18 can be exploited for positron emission tomography (PET) imaging ...