BIIB068 是一种有效，选择性，可逆和具有口服活性的 BTK 抑制剂，IC₅₀ 为 1 nM，K_d 为 0.3 nM。BIIB068 对 BTK 的选择性比其他激酶高 400 倍。BIIB068 可用于自身免疫性疾病的研究。

BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC 50 of 1 nM and a K d of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research.

Solid

IC50: 1 nM (BTK)
Kd: 0.3 nM (BTK)

BIIB068 (compound 1) improves the whole blood cell potency (human whole blood BTK phosphorylation (IC50 = 0.12 μM).
BIIB068 (compound 1; 30 μM,10 μM, 3.3 μM, and 1.1 μM) inhibits BCR mediated PLCγ2 phosphorylation in Ramos B cells (IC50= 0.4 μM), anti-IgD induced and anti-IgM BCR-induced B cell activation in human PBMCs (IC50 = 0.11 μM and 0.21 μM, respectively).
BIIB068 (compound 1) inhibits FcγR-mediated ROS production in neutrophils with an IC50 of 54 nM. has not independently confirmed the accuracy of these methods. They are for reference only.

BIIB068 (compound 1) is stable in the plasma of mouse, rat, beagle dog, and cynomolgus monkey (>95% parent compound remaining after 6 hours of incubation).
BIIB068 (compound 1) exhibits good drug-like properties (LLE = 5) which results in low in vivo clearance (CL %Q h = 6) and moderate oral bioavailability (%F = 48) when dosed in rats. BIIB068 (5 mg/kg; po) treatment shows the T 1/2 of 1.2 hours, 2.1 hours and 0.9 hour for rats, dog and cynomolgus monkey, respectively. BIIB068 shows acceptable ADME (absorption, distribution, metabolism, and excretion) properties. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Bin Ma, Tonika Bohnert, et al. Discovery of BIIB068: A Selective, Potent, Reversible Brutons Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases. J Med Chem. 2020 Jul 22.

In Vitro: DMSO : 31.25 mg/mL (71.75 mM; Need ultrasonic)配制储备液