OTS514 is a potent TOPK (T-LAK cell-originated protein kinase) inhibitor. OTS514 exhibits growth suppressive effect on small cell lung cancer. TS514 effectively suppressed growth of SCLC cell lines (IC50 ; 0.4 ~ 42.6 nM) and led to their apoptotic cell death. Treatment with OTS514 suppressed forkhead box protein M1 (FOXM1) activity, which was involved in stemness of CSC. Furthermore, OTS514 treatment reduced CD90-positive SCLC cells and showed higher cytotoxic effect against lung sphere-derived CSC-like SCLC cells.
CAS Number: 1338540-63-8
Molecular Weight: 364.46
Chemical Name: 9-[4-[(1R)-2-amino-1-methylethyl]phenyl]-8-hydroxy-6-methyl-thieno[2,3-c]quinolin-4(5H)-one hydrochloride
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138+ stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells.
OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells).
- Ikeda Y, Park JH, Miyamoto T, Takamatsu N, Kato T, Iwasa A, Okabe S, Imai Y, Fujiwara K, Nakamura Y, Hasegawa K. T-LAK Cell-Originated Protein Kinase (TOPK) as a Prognostic Factor and a Potential Therapeutic Target in Ovarian Cancer. Clin Cancer Res. 2016 Dec 15;22(24):6110-6117. PubMed PMID: 27334838.
- Park JH, Inoue H, Kato T, Zewde M, Miyamoto T, Matsuo Y, Salgia R, Nakamura Y. TOPK (T-LAK cell-originated protein kinase) inhibitor exhibits growth suppressive effect on small cell lung cancer. Cancer Sci. 2017 Jan 11. doi: 10.1111/cas.13160. [Epub ahead of print] PubMed PMID: 28075524.
- Kato T, Inoue H, Imoto S, Tamada Y, Miyamoto T, Matsuo Y, Nakamura Y, Park JH. Oncogenic roles of TOPK and MELK, and effective growth suppression by small molecular inhibitors in kidney cancer cells. Oncotarget. 2016 Apr 5;7(14):17652-64. doi: 10.18632/oncotarget.7755. PubMed PMID: 26933922; PubMed Central PMCID: PMC4951240.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.