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| 25mg |
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Purity: ≥98%
OTS964 HCl, the hydrochloride salt of OTS-964 and a dimethylated derivative of OTS 514, is a potent and selective inhibitor of TOPK (T-lymphokine-activated killer cell-originated protein kinase) with antitumor effects. With a high affinity and selectivity, it inhibits TOPK (IC50 = 28 nM). TOPK, a protein that is overexpressed in a number of cancers and tumors, is thought to function as an oncogene that encourages the growth of tumors. OTS964 may therefore have anticancer properties because it is a TOPK inhibitor. Both in vitro and in xenograft models of human lung cancer, it results in a cytokinesis defect and subsequent apoptosis of cancer cells. OTS964 administered as a liposomal formulation successfully caused total regression of transplanted tumors without causing any adverse reactions in mice, but it also caused hematopoietic adverse reactions (leukocytopenia associated with thrombocytosis).
| Targets |
TOPK (IC50 = 28 nM); CDK11B (IC50 = 40 nM)
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| ln Vitro |
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| ln Vivo |
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| Cell Assay |
At a specific density, 100 μl of cells are plated in 96-well plates. Prior to being exposed to compounds for 72 hours at 37°C, the cells are given an overnight period to adhere. At 450 nm in wavelength, plates are read using a spectrophotometer. Three duplicates of each assay are run. The z scores are computed to yield P values once the IC50 values have been measured. The log values of the IC50 for each of the 13 TOPK-positive cell lines are transformed to base ten (nM) and the mean and standard deviation are then computed.
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| Animal Protocol |
Nude mice bearing LU-99 lung cancer cells[1]
40 mg/kg Intravenously; on days 1, 4, 8, 11, 15, and 18 |
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| References |
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| Molecular Formula |
C23H24N2O2S.HCL
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| Molecular Weight |
428.98
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| Exact Mass |
428.1325269
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| Elemental Analysis |
C, 64.40; H, 5.87; Cl, 8.26; N, 6.53; O, 7.46; S, 7.47
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| CAS # |
1338545-07-5
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| Related CAS # |
OTS964;1338542-14-5
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| Appearance |
Solid powder
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| SMILES |
CC1=CC(=C(C2=C1NC(=O)C3=C2C=CS3)C4=CC=C(C=C4)[C@@H](C)CN(C)C)O.Cl
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| InChi Key |
YHPWOYBWUWSJDW-UQKRIMTDSA-N
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| InChi Code |
InChI=1S/C23H24N2O2S.ClH/c1-13-11-18(26)19(16-7-5-15(6-8-16)14(2)12-25(3)4)20-17-9-10-28-22(17)23(27)24-21(13)20;/h5-11,14,26H,12H2,1-4H3,(H,24,27);1H/t14-;/m0./s1
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| Chemical Name |
9-[4-[(2R)-1-(dimethylamino)propan-2-yl]phenyl]-8-hydroxy-6-methyl-5H-thieno[2,3-c]quinolin-4-one;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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.83 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 (5.83 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 (5.83 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 | 2.3311 mL | 11.6556 mL | 23.3111 mL | |
| 5 mM | 0.4662 mL | 2.3311 mL | 4.6622 mL | |
| 10 mM | 0.2331 mL | 1.1656 mL | 2.3311 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.
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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In vivoefficacy of OTS514 in ES-2 ovarian cancer peritoneal dissemination xenograft model.Clin Cancer Res.2016 Dec 15;22(24):6110-6117. |
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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