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BIIB068
CAS No. 1798787-27-5
BIIB068 ( —— )
产品货号. M23808 CAS No. 1798787-27-5
BIIB068 是一种选择性、可逆且具有口服活性的 BTK 抑制剂（IC50 = 1 nM，Kd = 0.3 nM）。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥1312 | 有现货 |
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| 10MG | ￥2203 | 有现货 |
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| 25MG | ￥3969 | 有现货 |
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| 50MG | ￥5970 | 有现货 |
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| 100MG | ￥7995 | 有现货 |
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| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称BIIB068
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述BIIB068 是一种选择性、可逆且具有口服活性的 BTK 抑制剂（IC50 = 1 nM，Kd = 0.3 nM）。
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产品描述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.
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体外实验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.
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体内实验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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同义词——
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通路Tyrosine Kinase
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靶点BTK
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受体BTK
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研究领域——
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适应症——
化学信息
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CAS Number1798787-27-5
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分子量435.52
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分子式C23H29N7O2
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纯度>98% (HPLC)
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溶解度DMSO:30mg/ml(68.88mM; Need ultrasonic)
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SMILESO=C(N1CC(OC(C)C)C1)NCC2=CC=C(C3=NC(NC4=CN(C)N=C4)=NC=C3)C=C2C
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Ma B , Bohnert T , Otipoby K L , et al. Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases[J]. Journal of Medicinal Chemistry, 2020, XXXX(XXX).
