OTS514

Name: OTS514
Brand: MedChemExpress
SKU: HY-18621
Rating: 5.0 (3 reviews)

Cat. No.: HY-18621 Purity: 99.77%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

OTS514 is a highly potent TOPK inhibitor with an IC₅₀ of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis.

For research use only. We do not sell to patients.

OTS514 Chemical Structure

CAS No. : 1338540-63-8

Size	Price	Stock	Quantity
2 mg	USD 115	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 530	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 730	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 997	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of OTS514:

(S)-OTS514 Get quote
OTS514 hydrochloride Get quote

3 Publications Citing Use of MCE OTS514

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

OTS514 is a highly potent TOPK inhibitor with an IC₅₀ of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells^[1]. OTS514 induces cell cycle arrest and apoptosis^[2].

IC₅₀ & Target

IC50: 2.6 nM (TOPK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
769-P	IC₅₀	20.7 nM Compound: OTS514	Cytotoxicity against human 769-P cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human 769-P cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 30108692]
786-0	IC₅₀	44.1 nM Compound: OTS514	Cytotoxicity against human 786-O cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human 786-O cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 30108692]
A2780	IC₅₀	10 nM Compound: OTS514	Cytotoxicity against human A2780 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human A2780 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
A549	IC₅₀	6.5 nM Compound: OTS514	Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
CAKI-1	IC₅₀	27.8 nM Compound: OTS514	Cytotoxicity against human Caki1 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human Caki1 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 30108692]
CAKI-2	IC₅₀	20.1 nM Compound: OTS514	Cytotoxicity against human Caki2 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human Caki2 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 30108692]
Caov-3 cell line	IC₅₀	5.1 nM Compound: OTS514	Cytotoxicity against human Caov3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human Caov3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
CWR22R	IC₅₀	8 nM Compound: OTS514	Cytotoxicity against human 22Rv1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human 22Rv1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
Daudi	IC₅₀	3.7 nM Compound: OTS514	Cytotoxicity against human Daudi cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human Daudi cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
DU-4475	IC₅₀	6.4 nM Compound: OTS514	Cytotoxicity against human DU4475 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human DU4475 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
HCT-116	IC₅₀	4.8 nM Compound: OTS514	Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
HepG2	IC₅₀	8.5 nM Compound: OTS514	Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
K562	IC₅₀	36.8 nM Compound: OTS514	Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
KG-1	IC₅₀	48.7 nM Compound: OTS514	Cytotoxicity against human KG1 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human KG1 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
KG-1a	IC₅₀	26.2 nM Compound: OTS514	Cytotoxicity against human KG1a cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human KG1a cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
Lu-99 cell line	IC₅₀	1.5 nM Compound: OTS514	Cytotoxicity against human LU99 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human LU99 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MDA-MB-231	IC₅₀	14 nM Compound: OTS514	Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MIA PaCa-2	IC₅₀	5.2 nM Compound: OTS514	Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MKN-1	IC₅₀	4.6 nM Compound: OTS514	Cytotoxicity against human MKN1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MKN1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MKN-45	IC₅₀	6.1 nM Compound: OTS514	Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
ML-2	IC₅₀	17.9 nM Compound: OTS514	Cytotoxicity against human ML2 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human ML2 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
MOLM-13	IC₅₀	9 nM Compound: OTS514	Cytotoxicity against human MOLM13 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human MOLM13 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
MV4-11	IC₅₀	10.7 nM Compound: OTS514	Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
OV-90	IC₅₀	8.8 nM Compound: OTS514	Cytotoxicity against human OV90 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human OV90 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
OVCAR-3	IC₅₀	12 nM Compound: OTS514	Cytotoxicity against human OVCAR3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human OVCAR3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
PA-1	IC₅₀	5 nM Compound: OTS514	Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
RMG-I	IC₅₀	15 nM Compound: OTS514	Cytotoxicity against human RMG-1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human RMG-1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
SK-OV-3	IC₅₀	6.3 nM Compound: OTS514	Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
SW626	IC₅₀	9.4 nM Compound: OTS514	Cytotoxicity against human SW626 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human SW626 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
T47D	IC₅₀	8.4 nM Compound: OTS514	Cytotoxicity against human T47D cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human T47D cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
THP-1	IC₅₀	23.5 nM Compound: OTS514	Cytotoxicity against human THP1 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human THP1 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
U-937	IC₅₀	19.2 nM Compound: OTS514	Cytotoxicity against human U937 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human U937 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
UMUC3	IC₅₀	5.7 nM Compound: OTS514	Cytotoxicity against human UM-UC-3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human UM-UC-3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]

In Vitro

OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138⁺ stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	Human myeloma cell lines (MM1.S, MM1.R, RPMI 8226, 8226Dox40, KMS34, KMS34CFZ, KMS11, JJN3, LP-1, NCI H929, U266B1)
Concentration:	1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 nM
Incubation Time:	72 hours
Result:	IC₅₀ values ranged from 11.6 to 29.4 nM in parental cell lines, indicating a potent inhibitory effect. Only the RPMI 8226-Dox40 cell line, which overexpresses the multi-drug resistance transporter gene ABCB1, is resistant.

In Vivo

OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells^[1]
Dosage:	1, 2.5, and 5 mg/kg
Administration:	Intravenously treated; once every day for 2 weeks
Result:	Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.

Molecular Weight

364.46

Formula

C₂₁H₂₀N₂O₂S

CAS No.

1338540-63-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NC2=C(C(C3=CC=C([C@@H](C)CN)C=C3)=C(O)C=C2C)C4=C1SC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 12 mg/mL (32.93 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7438 mL	13.7189 mL	27.4379 mL
5 mM	0.5488 mL	2.7438 mL	5.4876 mL
10 mM	0.2744 mL	1.3719 mL	2.7438 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (277 KB) SDS (392 KB)

COA (253 KB) HNMR (205 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[2]. Stefka AT, et al. Potent anti-myeloma activity of the TOPK inhibitor OTS514 in pre-clinical models. Cancer Med. 2020 Jan;9(1):324-334. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7438 mL	13.7189 mL	27.4379 mL	68.5946 mL
	5 mM	0.5488 mL	2.7438 mL	5.4876 mL	13.7189 mL
	10 mM	0.2744 mL	1.3719 mL	2.7438 mL	6.8595 mL
	15 mM	0.1829 mL	0.9146 mL	1.8292 mL	4.5730 mL
	20 mM	0.1372 mL	0.6859 mL	1.3719 mL	3.4297 mL
	25 mM	0.1098 mL	0.5488 mL	1.0975 mL	2.7438 mL
	30 mM	0.0915 mL	0.4573 mL	0.9146 mL	2.2865 mL

OTS514 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

OTS514

Customer Review

Other Forms of OTS514:

3 Publications Citing Use of MCE OTS514

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

OTS514 Related Classifications

Keywords:

Your Recently Viewed Products:

Name
Email *

	Sorry, but the email address you supplied was invalid.

OTS514

Customer Review

Other Forms of OTS514:

OTS514 Related Antibodies

3 Publications Citing Use of MCE OTS514

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

OTS514 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

OTS514 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report