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ONO-4059

Cat. No. M5333
ONO-4059 Structure
Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 170 In stock
25mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: The compound covalently bonds to BTK, inhibiting BCR signaling and B-cell proliferation and activation. NO/GS-4059 induced durable responses in relapsed/refractory B-cell malignancies without significant toxicities. In vivo: ONO-4059 demonstrated therapeutic efficacy in a mouse arthritis model, and based on its anti-proliferative activity in B-cells.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 454.48
Formula C25H22N6O3
CAS Number 1351636-18-4
Purity >99%
Solubility 10mM in DMSO
Storage at -20°C
References

PI3Kδ inhibitor idelalisib in combination with BTK inhibitor ONO/GS-4059 in diffuse large B cell lymphoma with acquired resistance to PI3Kδ and BTK inhibitors.
Yahiaoui A, et al. PLoS One. 2017 Feb 8;12(2):e0171221. PMID: 28178345.

A phase 1 clinical trial of the selective BTK inhibitor ONO/GS-4059 in relapsed and refractory mature B-cell malignancies.
Walter HS, et al. Blood. 2016 Jan 28;127(4):411-9. PMID: 26542378.

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ONO-4059 hydrochloride

ONO-4059 (GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.

ONO-4059 analogue

ONO-4059 analogue is the analog of ONO-4059, ONO-4059 is a highly potent and selective Btk inhibitor with IC50 of 23.9 nM.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ONO-4059 supplier, BTK, inhibitors

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