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MedKoo CAT#: 558256
CAS#: 1338540-63-8 (free base)
Description: 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.
MedKoo Cat#: 558256
Name: OTS514 HCl
CAS#: 1338540-63-8 (free base)
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
Related CAS #: 1338540-63-8 (free base) 1338544-87-8 (HBr) 1338541-25-5 (s-isomer) 1338545-92-8 (S-isomer HCl)
Synonym: OTS514; OTS 514; OTS-514; OTS514 HCl, OTS514 Hydrochloride.
IUPAC/Chemical Name: 9-[4-[(1R)-2-amino-1-methylethyl]phenyl]-8-hydroxy-6-methyl-thieno[2,3-c]quinolin-4(5H)-one hydrochloride
InChi Key: CQPRMBOOBXSZSP-YDALLXLXSA-N
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
SMILES Code: O=C1NC2=C(C(C3=CC=C([C@@H](C)CN)C=C3)=C(O)C=C2C)C4=C1SC=C4.[H]Cl
1: 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.
2: 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.
3: 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.
4: 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.