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Background Information:
TOPK (T–lymphokine-activated killer cell–originated protein kinase), an enzyme that is heavily and frequently transactivated in various cancer tissues, including lung and triple-negative breast cancers, plays a vital role in the mitosis of cancer cells. Optically pure OTS-964 is a TOPK small molecular inhibitor, binding to the enzyme potently and selectively with IC50 at lower nM. The inhibition causes a cytokinesis defect and the subsequent apoptosis of cancer cells in vitro as well as in xenograft models of human lung cancer. The drug delivered in a liposomal formulation effectively caused complete regression of transplanted tumors without any detectable side effects in mice (Ref. 1).
Reference:
1. Y. Matsuo, et al, TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis, Sci Transl Med, 22 October 2014, Vol. 6, Issue 259, p. 259ra145.
2. 100% R-enantiomer, clinically active isomer. All pharmacological parameters reported for this compound are based on a single optically pure entity. The product OTS-964 offered by Chemietek is good (in every aspect) for in vivo animal model studies.* Confirmed by third party with a high-precision quantitative elemental analysis.
APIM050056: OTS-964
CAS No.: 1338545-07-5.
Molecular Formula: C23H24N2O2S? H2O.
Molecular Weight: 410.5.
Purity: Refer to Certificate of Analysis, Batch-specific.
QC: HPLC-MS, 1HNMR, Chiral HPLC and Quatitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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