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BIIB068

CAS No. : 1798787-27-5

MCE 站：BIIB068

产品活性：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。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Btk

In Vitro: 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.

In Vivo: 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.

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  Ibrutinib-biotin  |  CG-806  |  LFM-A13  |  Ibrutinib deacryloylpiperidine  |  PCI 29732  |  Acalabrutinib D4

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