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.
Chemical Formula: C21H21ClN2O2S
Exact Mass: 364.1245
Molecular Weight: 400.921
Elemental Analysis: C, 62.91; H, 5.28; Cl, 8.84; N, 6.99; O, 7.98; S, 8.00
Chemical Name: 9-[4-[(1R)-2-amino-1-methylethyl]phenyl]-8-hydroxy-6-methyl-thieno[2,3-c]quinolin-4(5H)-one hydrochloride
InChi Code: InChI=1S/C21H20N2O2S.ClH/c1-11-9-16(24)17(14-5-3-13(4-6-14)12(2)10-22)18-15-7-8-26-20(15)21(25)23-19(11)18;/h3-9,12,24H,10,22H2,1-2H3,(H,23,25);1H/t12-;/m0./s1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
Alachkar H, Mutonga M, Malnassy G, Park JH, Fulton N, Woods A, Meng L, Kline J, Raca G, Odenike O, Takamatsu N, Miyamoto T, Matsuo Y, Stock W, Nakamura Y. T-LAK cell-originated protein kinase presents a novel therapeutic target in FLT3-ITD mutated acute myeloid leukemia. Oncotarget. 2015 Oct 20;6(32):33410-25. doi: 10.18632/oncotarget.5418. PubMed PMID: 26450903; PubMed Central PMCID: PMC4741775.
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