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Purity: ≥98%
OTS514 (OTS-514) is a novel TOPK (T-LAK cell-originated protein kinase) inhibitor with potential anticancer activity. Its IC50 of 2.6 nM provides TOPK inhibition. TOPK-positive cancer cells were significantly inhibited from growing. Additionally, with IC50 values ranging from 3.0 to 46 nM, it demonstrates a strong growth-inhibitory effect on ovarian cancer cell lines. At an IC50 between 0.4 and 42.6 nM, OTS514 exhibits growth-inhibiting properties against small cell lung cancer and can cause apoptosis in the affected cells. Additionally, the activity of the protein forkhead box protein M1 (FOXM1), which is essential for CSC stemness, was inhibited by OTS514. Furthermore, OTS514 treatment decreased CD90-positive SCLC cells and demonstrated increased cytotoxicity against CSC-like SCLC cells derived from lung spheres.
| Targets |
TOPK (IC50 = 2.6 nM)
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| ln Vivo |
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| Cell Assay |
The cells were cultivated in RPMI supplemented with 1×StemSpan CC100 and 20% fetal bovine serum. For 48 hours, cells were exposed to either OTS964 (100 or 200 nM) or OTS514 (20 or 40 nM). Following a PBS wash and resuspension in 100 milliliters of PBS, the collected cells were stained for 20 minutes at room temperature using CD41a antibody. Ultimately, the cells underwent one more PBS wash before being subjected to flow cytometry analysis for CD41a staining. Using an anti-STAT5 antibody, a Western blot was used to measure STAT5 expression.
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| Animal Protocol |
Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells[1]
1, 2.5, and 5 mg/kg Intravenously treated; once every day for 2 weeks |
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| References |
| Molecular Formula |
C21H20N2O2S
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| Molecular Weight |
364.46
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| Exact Mass |
364.13
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| Elemental Analysis |
C, 69.21; H, 5.53; N, 7.69; O, 8.78; S, 8.80
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| CAS # |
1338540-63-8
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| Related CAS # |
OTS514 hydrochloride;2319647-76-0
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| Appearance |
solid
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| SMILES |
CC1=CC(=C(C2=C1NC(=O)C3=C2C=CS3)C4=CC=C(C=C4)[C@@H](C)CN)O
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| InChi Key |
OETLNMOJNONWOY-LBPRGKRZSA-N
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| InChi Code |
InChI=1S/C21H20N2O2S/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)/t12-/m0/s1
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| Chemical Name |
9-[4-[(2R)-1-aminopropan-2-yl]phenyl]-8-hydroxy-6-methyl-5H-thieno[2,3-c]quinolin-4-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7438 mL | 13.7189 mL | 27.4379 mL | |
| 5 mM | 0.5488 mL | 2.7438 mL | 5.4876 mL | |
| 10 mM | 0.2744 mL | 1.3719 mL | 2.7438 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Growth-inhibitory and cytotoxic effects of OTS514 for ovarian cancer cells freshly-isolated from patients.Clin Cancer Res.2016 Dec 15;22(24):6110-6117. |
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In vivoefficacy of OTS514 in ES-2 ovarian cancer peritoneal dissemination xenograft model.Clin Cancer Res.2016 Dec 15;22(24):6110-6117. |
TOPK expression levels, IC50values to TOPK inhibitors and suppression of FOXM1 in ovarian cancer cell lines.Clin Cancer Res.2016 Dec 15;22(24):6110-6117. |
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