OTS514 hydrochloride

Catalog No.S7652 Batch:S765201

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Technical Data

Formula

C21H20N2O2S.HCl
Molecular Weight 400.92 CAS No. 2319647-76-0
Solubility (25°C)* In vitro DMSO 80 mg/mL (199.54 mM)
Water 80 mg/mL (199.54 mM)
Ethanol 5 mg/mL (12.47 mM)
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 4.000mg/ml (9.98mM)
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.650mg/ml (1.62mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description OTS514 is a highly potent TOPK(T-LAK cell-originated protein kinase) inhibitor with an IC50 value of 2.6 nM. OTS514 induces cell cycle arrest and apoptosis.
Targets
TOPK [2]
(Cell-free assay)
2.6 nM
In vitro OTS514 has growth inhibitory effect on five kidney cancer cell lines, VMRC-RCW, Caki-1, Caki-2, 769-P and 786-O, in which TOPK was highly expressed. The IC50 values range from 19.9 to 44.1 nM. OTS514 strongly suppressed the growth of TOPK-positive cancer cells. It also shows significant growth-inhibitory effect on ovarian cancer cell lines with IC50 values of 3.0 to 46 nM.
In vivo Mouse xenograft studies with human lung cancer cells demonstrated the in vivo efficacy of OTS514 but found that the compound also caused severe hematopoietic toxicity [reduction of red blood cells (RBCs) and white blood cells (WBCs) associated with marked increase in platelets]. Oral administration of OTS514 significantly elongated overall survival in the ES-2 abdominal dissemination xenograft model, compared with vehicle control (P < 0.001).

Protocol (from reference)

Cell Assay:[2]
  • Cell lines

    CD34+ HSCs

  • Concentrations

    20 or 40 nM

  • Incubation Time

    48 h

  • Method

    Cells were cultured in RPMI supplemented with 20% fetal bovine serum and 1×StemSpan CC100. Cells were treated with OTS514 (20 or 40 nM) or OTS964 (100 or 200 nM) for 48 hours. Collected cells were washed with PBS and resuspended in 100 ml of PBS followed by staining with CD41a antibody for 20 min at room temperature. Finally, the cells were washed with PBS again and then analyzed for CD41a staining by flow cytometry. Expression of STAT5 was examined by Western blot with an anti-STAT5 antibody.
Animal Study:[2]
  • Animal Models

    BALB/cSLC-nu/nu mice

  • Dosages

    1, 2.5, and 5 mg/kg

  • Administration

    IV or oral gavage

References

  • https://pubmed.ncbi.nlm.nih.gov/26933922/
  • https://pubmed.ncbi.nlm.nih.gov/25338756/
  • https://pubmed.ncbi.nlm.nih.gov/27334838/

Selleck's OTS514 hydrochloride Has Been Cited by 18 Publications

PBK, targeted by EVI1, promotes metastasis and confers cisplatin resistance through inducing autophagy in high-grade serous ovarian carcinoma [ Cell Death & Disease, February 18 2019, 166] PubMed: 30778048
TOPKi-NBD: a fluorescent small molecule for tumor imaging [ European Journal of Nuclear Medicine and Molecular Imaging, April 15 2020, 1003-1010] PubMed: 31734783
PDZ-binding kinase inhibitor OTS514 suppresses the proliferation of oral squamous carcinoma cells [ Oral Diseases, 2024 Mar, 30(2):223-234] PubMed: 36799330
PBK Enhances Cellular Proliferation With Histone H3 Phosphorylation and Suppresses Migration and Invasion With CDH1 Stabilization in Colorectal Cancer [ Frontiers in Pharmacology, 2022 Jan 18, 12:772926] PubMed: 35115926
PBK drives PARP inhibitor resistance through the TRIM37/NFκB axis in ovarian cancer [ Exp Mol Med, 2022, 54(7):999-1010] PubMed: 35859118
PBK phosphorylates MSL1 to elicit epigenetic modulation of CD276 in nasopharyngeal carcinoma [ Oncogenesis, 2021 Jan 5, 10(1):9] PubMed: 37938233
T-LAK cell-originated protein kinase (TOPK): an emerging prognostic biomarker and therapeutic target in osteosarcoma [ Molecular Oncology, 2021 Dec, 15(12):3721-3737] PubMed: 34115928
T-LAK cell-originated protein kinase (TOPK): an emerging prognostic biomarker and therapeutic target in osteosarcoma [ Mol Oncol, 2021, 15(12):3721-3737] PubMed: 34115928
PBK phosphorylates MSL1 to elicit epigenetic modulation of CD276 in nasopharyngeal carcinoma [ Oncogenesis, 2021, 10(1):9] PubMed: 33431797
PBK Enhances Cellular Proliferation With Histone H3 Phosphorylation and Suppresses Migration and Invasion With CDH1 Stabilization in Colorectal Cancer [ Front Pharmacol, 2021, 12:772926] PubMed: 35115926

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.