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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。


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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。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 371 | 现货 | |
| 5 mg | ¥ 893 | 现货 | |
| 10 mg | ¥ 1,480 | 现货 | |
| 25 mg | ¥ 2,380 | 现货 | |
| 50 mg | ¥ 3,490 | 现货 | |
| 100 mg | ¥ 4,720 | 现货 | |
| 200 mg | ¥ 6,360 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 978 | 现货 |
BIIB068 相关产品
| 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. |
| 靶点活性 | BTK:1 nM (IC50), BTK:0.3 nM (Kd) |
| 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. |
| 分子量 | 435.52 |
| 分子式 | C23H29N7O2 |
| CAS No. | 1798787-27-5 |
| Smiles | CC(C)OC1CN(C1)C(=O)NCc1ccc(cc1C)-c1ccnc(Nc2cnn(C)c2)n1 |
| 密度 | 1.30 g/cm3 (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 30 mg/mL (68.88 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.59 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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