BIIB068

Research use only, not for human use.

BIIB068 is an selective, reversible and orally active BTK inhibitor (IC50 = 1 nM, Kd = 0.3 nM).

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 (compound 1) improves the whole blood cell potency (humanwhole 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 anIC50 of 54 nM.

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 %Qh = 6) and moderate oral bioavailability (%F = 48) when dosed in rats. BIIB068 (5 mg/kg; po) treatment shows the T1/2 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.

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Tyrosine Kinase

BTK

BTK

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1798787-27-5

435.52

C23H29N7O2

>98% (HPLC)

DMSO:30mg/ml(68.88mM; Need ultrasonic)

O=C(N1CC(OC(C)C)C1)NCC2=CC=C(C3=NC(NC4=CN(C)N=C4)=NC=C3)C=C2C

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(-20℃)

With Ice Pack

≥ 2 years