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OTS964 hydrochloride

Catalog No. T4135 CAS 1338545-07-5

Synonyms: OTS964

OTS964 hydrochloride (OTS964) is a potent and selective TOPK inhibitor with potential anticancer activity.

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OTS964 hydrochloride, CAS 1338545-07-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 85.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 207.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 549.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 98.02%

Purity: 96.5%

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Description	OTS964 hydrochloride (OTS964) is a potent and selective TOPK inhibitor with potential anticancer activity.
Targets&IC50	TOPK:28 nM
In vitro	OTS964 inhibits the growth of TOPK-positive cells with low IC50 values [A549 (31 nM), LU-99 (7.6 nM), DU4475 (53 nM), MDAMB- 231 (73 nM), T47D (72 nM), Daudi (25 nM), UM-UC-3 (32 nM), HCT-116 (33 nM),MKN1 (38 nM), MKN45 (39 nM), HepG2 (19 nM), MIAPaca-2 (30 nM), and 22Rv1 (50 nM)], whereas its growth inhibitory effect against TOPK-negative HT29 cancer cells is significantly weaker, with IC50 of 290 nM. Although OTS964 reveals some suppressive effect on Src family kinases, the response to OTS964 in these cancer cells is not correlated with the expression of Src family kinases c-Src, Fyn, and Lyn, supporting the TOPK-dependent growth inhibitory effects of OTS964. Time lapse imaging in T47D cells shows that treatment with OTS964 induces cytokinesis defects followed by apoptosis
In vivo	Although administration of the free compound induces hematopoietic adverse reactions (leukocytopenia associated with thrombocytosis), the drug delivered in a liposomal formulation effectively causes complete regression of transplanted tumors without showing any adverse reactions in mice. Inhibition of TOPK activity with the liposomal OTS964 suppresses tumor growth through induction of cytokinesis defects and subsequent apoptosis. Although oral administration of OTS964 causes some hematopoietic toxicity, this is a transient effect. The spontaneous recovery from leukocytopenia is occured and the anticancer effectiveness of the oral drug is similar to that of the liposomal formulation, oral administration of the drug may prove to be more practical
Cell Research	Cell lines:?A549 cells, LU-99 cells, DU4475 cells, MDA-MB-231 cells, T47D cells, Daudi cells, UM-UC-3 cells, HCT-116 cells, MKN1 cells, MKN45 cells, HepG2 cells, MIAPaca-2 cells, 22Rv1 cells and HT29 cells Concentrations: --Incubation Time: 72 h Method: Cells (100 μl) are plated in 96-well plates at a certain density. The cells are allowed to adhere overnight before exposure to compounds for 72 hours at 37°C. Plates are read with a spectrophotometer at a wavelength of 450 nm. All assays are carried out in triplicate. After measuring IC50 values, we calculates the z scores to produce P values. After log transformation (base 10) of IC50 values (nM), the mean and SD are calculated for the log values of the IC50 for the 13 TOPK-positive cell lines.Method: Cells (100 μl) are plated in 96-well plates at a certain density. The cells are allowed to adhere overnight before exposure to compounds for 72 hours at 37°C. Plates are read with a spectrophotometer at a wavelength of 450 nm. All assays are carried out in triplicate. After measuring IC50 values, we calculates the z scores to produce P values. After log transformation (base 10) of IC50 values (nM), the mean and SD are calculated for the log values of the IC50 for the 13 TOPK-positive cell lines.
Animal Research	Animal Models: BALB/cSLC-nu/nu miceFormulation: 5% glucoseDosages: 40 mg/kgAdministration: i.v.

Synonyms	OTS964
Molecular Weight	428.97
Formula	C23H24N2O2S·HCl
CAS No.	1338545-07-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 1 mg/mL (2.33 mM)

DMSO: 79 mg/mL (184.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Matsuo Y, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145

Citations

1. Wang J, Luo L, Ding Q, et al. Development of a Multi-Target Strategy for the Treatment of Vitiligo via Machine Learning and Network Analysis Methods. Frontiers in pharmacology. 2021, 12.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Bioactive Compounds Library Max Anti-Pancreatic Cancer Compound Library Cell Cycle Compound Library Bioactive Compound Library Preclinical Compound Library MAPK Inhibitor Library HIF-1 Signaling Pathway Compound Library

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Keywords

OTS964 hydrochloride 1338545-07-5 Apoptosis Cell Cycle/Checkpoint MAPK CDK TOPK inhibit Inhibitor Cyclin dependent kinase OTS964 OTS-964 Hydrochloride OTS 964 OTS-964 hydrochloride OTS964 Hydrochloride OTS-964 OTS 964 Hydrochloride inhibitor

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