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Purity: ≥98%
OTS514 HCl (OTS 514; OTS-514), the hydrochloride salt of OTS514, is a novel and highly potent inhibitor of the TOPK (T-LAK cell-originated protein kinase) with potential antineoplastic activity. Its IC50 value of 2.6 nM indicates that it inhibits TOPK. The growth of TOPK-positive cancer cells was significantly suppressed by it. Moreover, it demonstrates a strong growth-inhibitory effect on ovarian cancer cell lines, with IC50 values ranging from 3.0 to 46 nM. OTS514 can cause apoptotic cell death in small cell lung cancer by exhibiting growth inhibitory effects, with an IC50 range of 0.4 ~ 42.6 nM. The activity of a protein involved in the stemness of CSC, forkhead box protein M1 (FOXM1), was also suppressed by OTS514. Additionally, OTS514 treatment exhibited increased cytotoxicity against lung sphere-derived CSC-like SCLC cells and decreased CD90-positive SCLC cells.
Targets |
TOPK (IC50 = 2.6 nM)
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ln Vitro |
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ln Vivo |
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Cell Assay |
The cells were cultivated in RPMI that was enhanced with 20% fetal bovine serum and 1×StemSpan CC100. For 48 hours, cells were exposed to OTS514 (20 or 40 nM) or OTS964 (100 or 200 nM). The collected cells underwent a PBS wash and were then resuspended in 100 milliliters of PBS. Subsequently, they were stained for 20 minutes at room temperature using CD41a antibody. Afterwards, the cells underwent one more PBS wash before being subjected to flow cytometry analysis for CD41a staining. Using an anti-STAT5 antibody on a Western blot, the expression of STAT5 was investigated.
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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.HCL
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Molecular Weight |
400.92
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Exact Mass |
364.12
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Elemental Analysis |
C, 62.91; H, 5.28; Cl, 8.84; N, 6.99; O, 7.98; S, 8.00
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CAS # |
2319647-76-0
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Related CAS # |
OTS514;1338540-63-8
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Appearance |
Solid powder
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SMILES |
CC1=CC(=O)C(=C2C1=NC(=O)C3=C2C=CS3)C4=CC=C(C=C4)C(C)CN.Cl
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InChi Key |
YCRRQRJUNVBPBW-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H18N2O2S.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;/h3-9,12H,10,22H2,1-2H3;1H
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Chemical Name |
9-[4-(1-aminopropan-2-yl)phenyl]-6-methylthieno[2,3-c]quinoline-4,8-dione;hydrochloride
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4943 mL | 12.4713 mL | 24.9426 mL | |
5 mM | 0.4989 mL | 2.4943 mL | 4.9885 mL | |
10 mM | 0.2494 mL | 1.2471 mL | 2.4943 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. th> |
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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. td> |
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. td> |