OTS514 hydrochloride

Catalog No.S7652 Batch:S765201

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)

	5% DMSO 1 95% Corn oil	0.65mg/ml
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.0mg/ml

* <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^[1]. 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^[3].

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]^[2]. Oral administration of OTS514 significantly elongated overall survival in the ES-2 abdominal dissemination xenograft model, compared with vehicle control (P < 0.001)^[3].

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

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

Selleck's OTS514 hydrochloride has been cited by 11 publications

PBK drives PARP inhibitor resistance through the TRIM37/NFκB axis in ovarian cancer [ Exp Mol Med, 2022, 54(7):999-1010]	PubMed: 35859118
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
PBK expression predicts favorable survival in colorectal cancer patients [ Virchows Arch, 2021, 10.1007/s00428-021-03062-0]	PubMed: 33638656
T-LAK cell-originated protein kinase (TOPK) is a Novel Prognostic and Therapeutic Target in Chordoma [ Cell Prolif, 2020, e12901]	PubMed: 32960500
PBK promotes aggressive phenotypes of cervical cancer through ERK/c-Myc signaling pathway [ J Cell Physiol, 2020, 10.1002/jcp.30134]	PubMed: 33184870
Novel Interleukin-6 Inducible Gene PDZ-Binding Kinase Promotes Tumor Growth of Multiple Myeloma Cells [ J Interferon Cytokine Res, 2020, 40(8):389-405]	PubMed: 32721246
TOPKi-NBD: a fluorescent small molecule for tumor imaging. [ Eur J Nucl Med Mol Imaging, 2019, 10.1007/s00259-019-04608-w]	PubMed: 31734783
PBK, targeted by EVI1, promotes metastasis and confers cisplatin resistance through inducing autophagy in high-grade serous ovarian carcinoma [ Cell Death Dis, 2019, 10(3):166]	PubMed: 30778048

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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.