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ONO-8430506

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Catalog No. T38759Cas No. 1354805-08-5

ONO-8430506 is an orally available, potent autotaxin (ATX)/ENPP2 inhibitor (IC90: 100 nM) that inhibits ATX activity in mouse plasma.

ONO-8430506

ONO-8430506

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Purity: 98.34%
Catalog No. T38759Cas No. 1354805-08-5
ONO-8430506 is an orally available, potent autotaxin (ATX)/ENPP2 inhibitor (IC90: 100 nM) that inhibits ATX activity in mouse plasma.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$111In StockIn Stock
5 mg$271In StockIn Stock
10 mg$375In StockIn Stock
25 mg$567In StockIn Stock
50 mg$763-In Stock
100 mg$1,020-In Stock
1 mL x 10 mM (in DMSO)$302In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.34%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
ONO-8430506 is an orally available, potent autotaxin (ATX)/ENPP2 inhibitor (IC90: 100 nM) that inhibits ATX activity in mouse plasma.
Targets&IC50
ATX/ENPP2:100 nM
In vitro
The IC50 values of ONO-8430506 against the lysophospholipase D (LysoPLD) activity of recombinant human ATX/ENPP2 are 5.1 nM and 4.5 nM, determined using synthetic fluorescent substrate (FS-3) and a natural substrate (16:0-LPC) assay, respectively.[2]
ONO-8430506 exhibits effective inhibition of lysophosphatidic acid (LPA) formation, demonstrating IC50 values of approximately 10 nM with both recombinant and plasma-derived ATX/ENPP2 derived from diverse animal species.[2]
In vivo
ONO-8430506 (10 mg/kg/day; gavage; for 21 days) initially slows tumor growth and limits lung metastasis, with tumor size comparable to the vehicle group by day 13. It reduces the initial phase of breast tumor growth and lung metastases by ~60% in a syngeneic orthotopic mouse model. ONO-8430506 (oral; 30 mg/kg) demonstrates good pharmacokinetics and persistently inhibits plasma lysophosphatidic acid formation in rats. Additionally, ONO-8430506 (30 or 100 mg/kg) enhances the antitumor effect of Paclitaxel in a breast cancer model. The compound exhibits moderate oral bioavailability (rat 51.6%, dog 71.1%, monkey 30.8%) and Cmax (rat 261, dog 1670, monkey 63 ng/mL) following oral administration (rat 1, dog 1, and monkey 1 mg/kg).
Chemical Properties
Molecular Weight461.53
FormulaC27H28FN3O3
Cas No.1354805-08-5
SmilesOC(=O)C12CCC(CC(=O)N3CCc4c(C3)n(Cc3ccc(F)cc3)c3ncccc43)(CC1)C2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 90 mg/mL (195 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.15 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1667 mL10.8335 mL21.6671 mL108.3353 mL
5 mM0.4333 mL2.1667 mL4.3334 mL21.6671 mL
10 mM0.2167 mL1.0834 mL2.1667 mL10.8335 mL
20 mM0.1083 mL0.5417 mL1.0834 mL5.4168 mL
50 mM0.0433 mL0.2167 mL0.4333 mL2.1667 mL
100 mM0.0217 mL0.1083 mL0.2167 mL1.0834 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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