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Tirabrutinib (ONO-4059)

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

Tirabrutinib; GS-4059; Velexbru

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 85  USD85 In stock
25mg USD 150  USD150 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 454.48
Formula C25H22N6O3
CAS Number 1351636-18-4
Solubility (25°C) 10mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Yahiaoui A, et al. PLoS One. 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.

[2] Walter HS, et al. Blood. A phase 1 clinical trial of the selective BTK inhibitor ONO/GS-4059 in relapsed and refractory mature B-cell malignancies.

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


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