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ONO-8430506

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

Purity: 97.05%
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 SizePriceAvailabilityQuantity
1 mg$263In Stock
5 mg$645In Stock
10 mg$892In Stock
25 mg$1,350In Stock
50 mg$1,820In Stock
100 mg$2,450In Stock
1 mL x 10 mM (in DMSO)$718In Stock
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Purity:97.05%
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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
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 90.0 mg/mL (195.0 mM), Sonication is recommended.
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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