化合物BIIB068 T9192
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Product IntroductionBioactivity英文名: BIIB068描述: BIIB068 是可逆的、选择性的、具有口服活性的 BTK 抑制剂 (IC50:1 nM;Kd:0.3 nM)。它对 BTK 的选择性比其他激酶高
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Product Introduction
Bioactivity
英文名: BIIB068
描述: BIIB068 是可逆的、选择性的、具有口服活性的 BTK 抑制剂 (IC50:1 nM;Kd:0.3 nM)。它对 BTK 的选择性比其他激酶高 400 倍。它可用于自身免疫性疾病的研究。
体外活性: BIIB068 inhibits B cell, neutrophil and monocyte activation in vitro, but not T cell responses.
体内活性: BIIB068 demonstrated good PK/PD correlation with in vivo EC50 = 0.16 μM based on antibody esponse, similar to in vivo WB pBTK potency in mice. BIIB068 exhibited no adverse effects in the single dose CNS and respiratory studies in rats nor in a single dose cardiovascular study in monkeys. BIIB068 was well tolerated and effective at inhibiting BTK phosphorylation in healthy subjects.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 30 mg/mL(68.88 mM)
关键字: ADME | inhibit | FcγR | Autoimmune | Bruton tyrosine kinase | TNFα | BIIB 068 | BIIB068 | BIIB-068 | ROS | Inhibitor | reversible | Btk | anti-IgD | phosphorylation | anti-IgM
相关产品: JAK3/BTK-IN-2 | BTK-IN-25 | LFM-A13 | Rilzabrutinib | zanubrutinib | BMS-935177 | (Rac)-IBT6A | TAK-020 | Avitinib | Acalabrutinib enantiomer
相关库: Drug Repurposing Compound Library | Angiogenesis related Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library
Bioactivity
英文名: BIIB068
描述: BIIB068 是可逆的、选择性的、具有口服活性的 BTK 抑制剂 (IC50:1 nM;Kd:0.3 nM)。它对 BTK 的选择性比其他激酶高 400 倍。它可用于自身免疫性疾病的研究。
体外活性: BIIB068 inhibits B cell, neutrophil and monocyte activation in vitro, but not T cell responses.
体内活性: BIIB068 demonstrated good PK/PD correlation with in vivo EC50 = 0.16 μM based on antibody esponse, similar to in vivo WB pBTK potency in mice. BIIB068 exhibited no adverse effects in the single dose CNS and respiratory studies in rats nor in a single dose cardiovascular study in monkeys. BIIB068 was well tolerated and effective at inhibiting BTK phosphorylation in healthy subjects.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 30 mg/mL(68.88 mM)
关键字: ADME | inhibit | FcγR | Autoimmune | Bruton tyrosine kinase | TNFα | BIIB 068 | BIIB068 | BIIB-068 | ROS | Inhibitor | reversible | Btk | anti-IgD | phosphorylation | anti-IgM
相关产品: JAK3/BTK-IN-2 | BTK-IN-25 | LFM-A13 | Rilzabrutinib | zanubrutinib | BMS-935177 | (Rac)-IBT6A | TAK-020 | Avitinib | Acalabrutinib enantiomer
相关库: Drug Repurposing Compound Library | Angiogenesis related Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library
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