BIIB068 是可逆的、选择性的、具有口服活性的BTK抑制剂 (IC50:1 nM;Kd:0.3 nM)。它对BTK的选择性比其他激酶高 400 倍。它可用于自身免疫性疾病的研究。

BIIB068 is an selective, reversible and orally active BTK inhibitor (IC50 = 1 nM, Kd = 0.3 nM). BIIB068 is 400 times more selective for BTK than other kinases.

BIIB068 inhibits B cell, neutrophil and monocyte activation in vitro, but not T cell responses.

BIIB068 demonstrated good PK/PD correlation with in vivo EC50 = 0.16 μM based on antibody esponse, similar to in vivo WB pBTK potency in mice. BIIB068 exhibited no adverse effects in the single dose CNS and respiratory studies in rats nor in a single dose cardiovascular study in monkeys. BIIB068 was well tolerated and effective at inhibiting BTK phosphorylation in healthy subjects.

1798787-27-5

C23H29N7O2

435.532

DMSO:30mg/ml(68.88mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years