BIIB068 |
Katalog-Nr.GC60643 |
BIIB068 ist ein potenter, selektiver, reversibler und oral aktiver BTK-Inhibitor mit einem IC50 von 1 nM und einem Kd von 0,3 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1798787-27-5
Sample solution is provided at 25 µL, 10mM.
BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research[1].
BIIB068 (compound 1) improves the whole blood cell potency (human whole blood BTK phosphorylation (IC50 = 0.12 µM)[1]. 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)[1]. BIIB068 (compound 1) inhibits FcγR-mediated ROS production in neutrophils with an IC50 of 54 nM[1].
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)[1].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[1].
[1]. Bin Ma, Tonika Bohnert, et al. Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases. J Med Chem. 2020 Jul 22.
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