ONO-8430506

SKU: orb1691793

Description

ONO-8430506 is a potent and orally bioavailable inhibitor of autotaxin (ATX/ENPP2), demonstrating an IC90 of 100 nM. It effectively suppresses ATX activity in mouse plasma and is a valuable research tool for investigating lysophosphatidic acid (LPA) signaling in cancer, fibrosis, and inflammation research, both in vitro and in vivo.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1354805-08-5
• MW: 461.53
• Purity: 98.34% (May vary between batches)
• Formula: C₂₇H₂₈FN₃O₃
• SMILES: OC(=O)C12CCC(CC(=O)N3CCc4c(C3)n(Cc3ccc(F)cc3)c3ncccc43)(CC1)C2
• Target: PDE
• Solubility: DMSO:90 mg/mL (195 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.15 mM)

Bioactivity

• Target IC50:
  ATX/ENPP2:100 nM
• 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).
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• 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ONO8430506, ONO-8430506, ONO 8430506, enpp, ATX (autotaxin)

Compound Identifiers

PubChem CID

56597976