1351636-18-4
中文名称
替拉鲁替尼
英文名称
Btk Kinase inhibitor
CAS
1351636-18-4
分子式
C25H22N6O3
分子量
454.48
MOL 文件
1351636-18-4.mol
更新日期
2024/05/28 11:53:43
1351636-18-4 结构式
基本信息
中文别名
替拉鲁替尼(R)-6-氨基-9-(1-(丁-2-炔酰基)吡咯烷-3-基)-7-(4-苯氧基苯基)-7H-嘌呤-8(9H)-酮
英文别名
ONO-BKTONO BTK
Tirabrutinib
TIRABRUTINIB
GS-4059
Btk Kinase inhibitor
ONO-4059(Tirabrutinib)
Tirabrutinib (ONO-4059)
ONO-4059
ONO 4059
ONO4059
ONO-4059(GS-4059,Tirabrutinib) free base
ONO-4059
ONO4059
ONO 4059
ONO-4059
GS 4059
GS-4059
GS4059
ONO-WG-307
TIRABRUTINIB
所属类别
生物化工：抑制剂物理化学性质
沸点672.0±65.0 °C(Predicted)
密度1.412±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO:65.0(Max Conc. mg/mL);143.02(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.66(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);66.01(Max Conc. mM)
Ethanol:1.0(Max Conc. mg/mL);2.2(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.66(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);66.01(Max Conc. mM)
Ethanol:1.0(Max Conc. mg/mL);2.2(Max Conc. mM)
酸度系数(pKa)3.16±0.20(Predicted)
形态结晶固体
应用领域
用途1
一种有效的口服活性的BTK(布鲁顿酪氨酸激酶)抑制剂, IC50:2.2nM。Tirabrutinib is a potent and orally active Bruton agammaglobulinemia tyrosine kinase (BTK) in hibitor. Upon administration, ONO-4059 covalently binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. As a result, this agent may inhibit the proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.