产品
编 号：F131793
分子式：C25H22N6O3
分子量：454.48
分子式：C25H22N6O3
分子量：454.48
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1351636-18-4
产品详情
生物活性：
Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.
体内研究：
Tirabrutinib (10 mg/kg; p.o.; single) is rapidly absorbed into plasma and brain, and reaches Cmax (blood Cmax =339.53 ng/mL; brain Cmax =28.9 ng/mL) 2 hours post administration.Tirabrutinib (6, 20 mg/kg; p.o.; single daily for 3 weeks) shows inhibition of tumour growth in vivo.Animal Model:Male SD rats (219.0–260.5g).
Dosage:10 mg/kg
Administration:Oral administration; single.
Result:1.19Pharmacokinetic Parameters of Tirabrutinib in male SD rats.Plasma, Cmax (ng/mL)Brain, Cmax (ng/mL)Penetration rate(%, Cmax,brain/Cmax,plasma)
PO (10 mg/kg)339.5328.98.5
Animal Model:Immunodeficiency (SCID) mice (mouse xenograft model).
Dosage:6, 20 mg/kg
Administration:Oral administration; single daily for 3 weeks.
Result:Inhibited tumour growth, and when dosage up to 20 mg/kg, a complete tumor suppression at day 14.
体外研究：
Tirabrutinib (0.1-1000 nM or 0.001-100 nM; 72 h) inhibits the proliferation of OCI-L Y10 and SU-DHL-6 cells with IC50s of 9.127 nM, and 17.10 nM, respectively.Tirabrutinib (0.5, 5, 50 μM; 24, 48 h) induces SU-DHL-6 cells apoptosis needs high dosage and prolonged administration (concentration up to 50 μM and incubates for 48 h).Tirabrutinib (300 nM, 72 h) induces caspase-3 and PARP cleavage in TMD8 cells.
Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.
体内研究：
Tirabrutinib (10 mg/kg; p.o.; single) is rapidly absorbed into plasma and brain, and reaches Cmax (blood Cmax =339.53 ng/mL; brain Cmax =28.9 ng/mL) 2 hours post administration.Tirabrutinib (6, 20 mg/kg; p.o.; single daily for 3 weeks) shows inhibition of tumour growth in vivo.Animal Model:Male SD rats (219.0–260.5g).
Dosage:10 mg/kg
Administration:Oral administration; single.
Result:1.19Pharmacokinetic Parameters of Tirabrutinib in male SD rats.Plasma, Cmax (ng/mL)Brain, Cmax (ng/mL)Penetration rate(%, Cmax,brain/Cmax,plasma)
PO (10 mg/kg)339.5328.98.5
Animal Model:Immunodeficiency (SCID) mice (mouse xenograft model).
Dosage:6, 20 mg/kg
Administration:Oral administration; single daily for 3 weeks.
Result:Inhibited tumour growth, and when dosage up to 20 mg/kg, a complete tumor suppression at day 14.
体外研究：
Tirabrutinib (0.1-1000 nM or 0.001-100 nM; 72 h) inhibits the proliferation of OCI-L Y10 and SU-DHL-6 cells with IC50s of 9.127 nM, and 17.10 nM, respectively.Tirabrutinib (0.5, 5, 50 μM; 24, 48 h) induces SU-DHL-6 cells apoptosis needs high dosage and prolonged administration (concentration up to 50 μM and incubates for 48 h).Tirabrutinib (300 nM, 72 h) induces caspase-3 and PARP cleavage in TMD8 cells.
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