ON-013100

Name: ON-013100
Brand: MedChemExpress
SKU: HY-112822
Rating: 5.0 (2 reviews)

Cat. No.: HY-112822 Purity: 98.66%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

ON-013100, an antineoplastic agent, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.

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

ON-013100 Chemical Structure

CAS No. : 865783-95-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 620	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 920	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of ON-013100:

Briciclib In-stock

2 Publications Citing Use of MCE ON-013100

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•Related Screening Libraries:

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View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Purity & Documentation
References
Customer Review

Description

ON-013100, an antineoplastic agent, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.

IC₅₀ & Target^[1]

Cdk4/cyclin D1

Cellular Effect

Cell Line	Type	Value	Description	References
2008	IC₅₀	0.005 μM Compound: 6aa	Antitumor activity against human 2008 cells by trypan blue exclusion assay Antitumor activity against human 2008 cells by trypan blue exclusion assay	[PMID: 18088089]
A549	IC₅₀	0.01 μM Compound: 6aa	Antitumor activity against human A549 cells by trypan blue exclusion assay Antitumor activity against human A549 cells by trypan blue exclusion assay	[PMID: 18088089]
AGS	IC₅₀	0.007 μM Compound: 6aa	Antitumor activity against human AGS cells by trypan blue exclusion assay Antitumor activity against human AGS cells by trypan blue exclusion assay	[PMID: 18088089]
BT-20	IC₅₀	0.01 μM Compound: 6aa	Antitumor activity against human BT20 cells by trypan blue exclusion assay Antitumor activity against human BT20 cells by trypan blue exclusion assay	[PMID: 18088089]
CCRF-CEM	IC₅₀	0.009 μM Compound: 6aa	Antitumor activity against human CEM cells by trypan blue exclusion assay Antitumor activity against human CEM cells by trypan blue exclusion assay	[PMID: 18088089]
CCRF-CEM	IC₅₀	0.01 μM Compound: 6aa	Antitumor activity against human CEM cells by trypan blue exclusion assay Antitumor activity against human CEM cells by trypan blue exclusion assay	[PMID: 18088089]
CEM/C2	IC₅₀	0.01 μM Compound: 6aa	Antitumor activity against human multidrug-resistant CEM/C2 cells by trypan blue exclusion assay Antitumor activity against human multidrug-resistant CEM/C2 cells by trypan blue exclusion assay	[PMID: 18088089]
COLO 205	IC₅₀	0.009 μM Compound: 6aa	Antitumor activity against human COLO205 cells by trypan blue exclusion assay Antitumor activity against human COLO205 cells by trypan blue exclusion assay	[PMID: 18088089]
Daudi	IC₅₀	0.007 μM Compound: 6aa	Antitumor activity against human Daudi cells by trypan blue exclusion assay Antitumor activity against human Daudi cells by trypan blue exclusion assay	[PMID: 18088089]
DLD-1	IC₅₀	0.003 μM Compound: 6aa	Antitumor activity against human DLD1 cells by trypan blue exclusion assay Antitumor activity against human DLD1 cells by trypan blue exclusion assay	[PMID: 18088089]
DU-145	IC₅₀	0.003 μM Compound: 6aa	Antitumor activity against AR-negative human DU145 cells by trypan blue exclusion assay Antitumor activity against AR-negative human DU145 cells by trypan blue exclusion assay	[PMID: 18088089]
HCT-116	IC₅₀	0.009 μM Compound: 6aa	Antitumor activity against human HCT116 cells by trypan blue exclusion assay Antitumor activity against human HCT116 cells by trypan blue exclusion assay	[PMID: 18088089]
HCT-15	IC₅₀	0.008 μM Compound: 6aa	Antitumor activity against human HCT15 cells by trypan blue exclusion assay Antitumor activity against human HCT15 cells by trypan blue exclusion assay	[PMID: 18088089]
K562	IC₅₀	0.004 μM Compound: 6aa	Antitumor activity against human K562 cells by trypan blue exclusion assay Antitumor activity against human K562 cells by trypan blue exclusion assay	[PMID: 18088089]
MCF7	IC₅₀	0.004 μM Compound: 6aa	Antitumor activity against ER-positive human MCF7 cells by trypan blue exclusion assay Antitumor activity against ER-positive human MCF7 cells by trypan blue exclusion assay	[PMID: 18088089]
MES-SA	IC₅₀	0.006 μM Compound: 6aa	Antitumor activity against human MES-SA cells by trypan blue exclusion assay Antitumor activity against human MES-SA cells by trypan blue exclusion assay	[PMID: 18088089]
MES-SA/Dx5	IC₅₀	0.005 μM Compound: 6aa	Antitumor activity against human multidrug-resistant MES-SA/DX5 cells by trypan blue exclusion assay Antitumor activity against human multidrug-resistant MES-SA/DX5 cells by trypan blue exclusion assay	[PMID: 18088089]
MIA PaCa-2	IC₅₀	0.004 μM Compound: 6aa	Antitumor activity against human MiaPaCa2 cells by trypan blue exclusion assay Antitumor activity against human MiaPaCa2 cells by trypan blue exclusion assay	[PMID: 18088089]
MOLT-4	IC₅₀	0.005 μM Compound: 6aa	Antitumor activity against human MOLT4 cells by trypan blue exclusion assay Antitumor activity against human MOLT4 cells by trypan blue exclusion assay	[PMID: 18088089]
NAMALVA	IC₅₀	0.006 μM Compound: 6aa	Antitumor activity against human Namalwa cells by trypan blue exclusion assay Antitumor activity against human Namalwa cells by trypan blue exclusion assay	[PMID: 18088089]
NCI-H187	IC₅₀	0.007 μM Compound: 6aa	Antitumor activity against human H187 cells by trypan blue exclusion assay Antitumor activity against human H187 cells by trypan blue exclusion assay	[PMID: 18088089]
OVCAR-3	IC₅₀	0.006 μM Compound: 6aa	Antitumor activity against human OVCAR-3 cells by trypan blue exclusion assay Antitumor activity against human OVCAR-3 cells by trypan blue exclusion assay	[PMID: 18088089]
PC-3	IC₅₀	0.008 μM Compound: 6aa	Antitumor activity against AR-positive human PC3 cells by trypan blue exclusion assay Antitumor activity against AR-positive human PC3 cells by trypan blue exclusion assay	[PMID: 18088089]
Raji	IC₅₀	0.004 μM Compound: 6aa	Antitumor activity against human Raji cells by trypan blue exclusion assay Antitumor activity against human Raji cells by trypan blue exclusion assay	[PMID: 18088089]
SK-MEL-28	IC₅₀	0.007 μM Compound: 6aa	Antitumor activity against human SK-MEL-28 cells by trypan blue exclusion assay Antitumor activity against human SK-MEL-28 cells by trypan blue exclusion assay	[PMID: 18088089]
SK-OV-3	IC₅₀	0.006 μM Compound: 6aa	Antitumor activity against human SKOV3 cells by trypan blue exclusion assay Antitumor activity against human SKOV3 cells by trypan blue exclusion assay	[PMID: 18088089]
SW480	IC₅₀	0.007 μM Compound: 6aa	Antitumor activity against human SW480 cells by trypan blue exclusion assay Antitumor activity against human SW480 cells by trypan blue exclusion assay	[PMID: 18088089]
T47D	IC₅₀	0.006 μM Compound: 6aa	Antitumor activity against ER-positive human T47D cells by trypan blue exclusion assay Antitumor activity against ER-positive human T47D cells by trypan blue exclusion assay	[PMID: 18088089]
U-87MG ATCC	IC₅₀	0.007 μM Compound: 6aa	Antitumor activity against human U87 cells by trypan blue exclusion assay Antitumor activity against human U87 cells by trypan blue exclusion assay	[PMID: 18088089]

In Vitro

ON-013100 induces apoptosis, and has activity against most human cancer cell lines in vitro. ON013100 significantly alters the cell cycle profile, dramatically increasing the number of cells in G2/M phase. Treatment of the cells with even 0.1 μM of ON013100 results in an arrest of the G2/M phase of the cell cycle^[2]. ON 013100 inhibits the proliferation of MCL (JEKO-1 and MINO), breast (MCF7 and MDA-MB-231), gastric (AGS), and esophageal (OE19, OE33, and FLO-1) cancer cell lines at a nanomolar concentration (ON 013100 GI₅₀=6.7-11.2 nM) ^[3].

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

Molecular Weight

394.44

Formula

C₁₉H₂₂O₇S

CAS No.

865783-95-5

Appearance

Solid

Color

White to off-white

SMILES

OC1=CC(CS(=O)(/C=C/C2=C(OC)C=C(OC)C=C2OC)=O)=CC=C1OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (63.38 mM; Need ultrasonic; 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	2.5352 mL	12.6762 mL	25.3524 mL
5 mM	0.5070 mL	2.5352 mL	5.0705 mL
10 mM	0.2535 mL	1.2676 mL	2.5352 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: 1.25 mg/mL (3.17 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 1.25 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: 1.25 mg/mL (3.17 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.

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: 98.66%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (248 KB) HNMR (142 KB) RP-HPLC (437 KB) MS (98 KB)

Handling Instructions (2659 KB)

References

[1]. Cho SY, et al. Determination of the glucuronide metabolite of ON 013100, a benzylstyrylsulfone antineoplastic drug, in colon cancer cells using LC/MS/MS. J Pharm Biomed Anal. 2013 Mar 5;75:138-44. [Content Brief]

[2]. Park IW, et al. Evaluation of novel cell cycle inhibitors in mantle cell lymphoma. Oncogene. 2007 Aug 16;26(38):5635-42. [Content Brief]

[3]. Neel Jasani, et al. Potent anticancer activity of an orally bioavailable small molecule, ON 013100, and its water soluble derivative, briciclib, a clinical-stage eIF4E-targeted agent. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.5352 mL	12.6762 mL	25.3524 mL	63.3810 mL
	5 mM	0.5070 mL	2.5352 mL	5.0705 mL	12.6762 mL
	10 mM	0.2535 mL	1.2676 mL	2.5352 mL	6.3381 mL
	15 mM	0.1690 mL	0.8451 mL	1.6902 mL	4.2254 mL
	20 mM	0.1268 mL	0.6338 mL	1.2676 mL	3.1690 mL
	25 mM	0.1014 mL	0.5070 mL	1.0141 mL	2.5352 mL
	30 mM	0.0845 mL	0.4225 mL	0.8451 mL	2.1127 mL
	40 mM	0.0634 mL	0.3169 mL	0.6338 mL	1.5845 mL
	50 mM	0.0507 mL	0.2535 mL	0.5070 mL	1.2676 mL
	60 mM	0.0423 mL	0.2113 mL	0.4225 mL	1.0563 mL

ON-013100 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.

Keywords:

ON-013100865783-95-5ON013100ON 013100CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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ON-013100

Customer Review

Other Forms of ON-013100:

ON-013100 Related Antibodies

2 Publications Citing Use of MCE ON-013100

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

ON-013100 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

ON-013100 Related Classifications

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