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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).
Catalog NO: CT-OTS964
Synonym: OTS964
CAS NO: 1338545-07-5
Mol. Formula: C23H24N2O2S∙ H2O
MW: 410.5
** in vivo Quality Material. 99.8-100% by achiral and chiral HPLCs. A snow-white crystalline powder (pic attached). Monohydrate (salt free)*, validated by a spot-on microanalysis. Bulk Stock!! Prompt.