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Tirabrutinib (ONO-4059)

Cat. No. M5333
Tirabrutinib (ONO-4059) Structure

Tirabrutinib; GS-4059; Velexbru

Size Price Availability Quantity
5mg USD 90  USD100 In stock
10mg USD 153  USD170 In stock
25mg USD 270  USD300 In stock
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Quality Control
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 454.48
Formula C25H22N6O3
CAS Number 1351636-18-4
Purity >98%
Solubility 10mM in DMSO
Storage at -20°C

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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Keywords: Tirabrutinib (ONO-4059), Tirabrutinib; GS-4059; Velexbru supplier, BTK, inhibitors

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