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ONO-8430506

Catalog No. T38759   CAS 1354805-08-5

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

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ONO-8430506 Chemical Structure
ONO-8430506, CAS 1354805-08-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 313.00
5 mg In stock $ 763.00
10 mg In stock $ 1,070.00
25 mg In stock $ 1,590.00
50 mg In stock $ 2,130.00
100 mg In stock $ 2,890.00
1 mL * 10 mM (in DMSO) In stock $ 892.00
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Purity: 97.05%
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Biological Description
Chemical Properties
Storage & Solubility Information
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). Tumor growth in ONO-8430506-treated mice caught up to the vehicle group by day 13; thereafter, primary tumor size was not significantly different from the vehicle-treated mice. It can slows initial tumor growth and limits lung metastasis. ONO-8430506 decreases the initial phase of breast tumor growth and subsequent lung metastases by ~60% in a syngeneic orthotopic mouse model.[1]
ONO-8430506 (oral; 30 mg/kg) demonstrates good pharmacokinetics and persistently inhibits plasma lysophosphatidic acid formation in rats.[2]
ONO-8430506 (30 or 100 mg/kg) enhances the antitumor effect of Paclitaxel in a breast cancer model.[3]
ONO-8430506 exhibits moderate oral bioavailability (rat 51.6%, dog 71.1%, and monkey 30.8%) and C max (rat 261, dog 1670, and monkey 63 ng/mL) following oral administration (rat 1, dog 1, and monkey 1 mg/kg).[3]
Molecular Weight 461.53
Formula C27H28FN3O3
CAS No. 1354805-08-5

Storage

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

Solubility Information

DMSO: 90.0 mg/mL (195.0 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Matthew G K Benesch, et al. Inhibition of autotaxin delays breast tumor growth and lung metastasis in mice. FASEB J. 2014;28(6):2655-2666. 2. Hiroshi Saga, et al. A novel highly potent autotaxin/ENPP2 inhibitor produces prolonged decreases in plasma lysophosphatidic acid formation in vivo and regulates urethral tension. PLoS One. 2014;9(4):e93230. 3. Yuzo Iwaki, et al. ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model. ACS Med Chem Lett. 2020;11(6):1335-1341.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

ONO-8430506 1354805-08-5 Metabolism PDE ONO 8430506 ONO8430506 inhibitor inhibit

 

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