OTS-964

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.