Tirabrutinib,1439901-97-9

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Tirabrutinib hydrochloride

CAS No. : 1439901-97-9

MCE 国际站：Tirabrutinib hydrochloride

产品活性：Tirabrutinib (ONO-4059) hydrochloride 是一种口服有效的高选择性 Bruton’s Tyrosine Kinase (BTK) 抑制剂 (能透过血脑屏障)，其 IC₅₀ 值为 6.8 nM。Tirabrutinib hydrochloride 不可逆共价结合 BTK 并抑制异常 B 细胞受体信号传导。Tirabrutinib hydrochloride 可用于自身免疫性疾病和血液学恶性肿瘤的研究。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：Btk  |  Apoptosis

In Vitro: Tirabrutinib hydrochloride (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 hydrochloride (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 hydrochloride (300 nM, 72 h) induces caspase-3 and PARP cleavage in TMD8 cells.

In Vivo: Tirabrutinib hydrochloride (10 mg/kg; p.o.; single) is rapidly absorbed into plasma and brain, and reaches C_max (blood C_max =339.53 ng/mL; brain C_max =28.9 ng/mL) 2 hours post administration.
Tirabrutinib hydrochloride (6, 20 mg/kg; p.o.; single daily for 3 weeks) shows inhibition of tumour growth in vivo.

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