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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 |
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:0.3 nM (Kd), BTK:1 nM (IC50) |
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) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 30 mg/mL (68.88 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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