产品
编 号：F601341
分子式：C23H29N7O2
分子量：435.52
分子式：C23H29N7O2
分子量：435.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1798787-27-5
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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 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.
体内研究：
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.
体外研究：
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.
产品资料
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