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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $40 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $163 | In Stock | |
25 mg | $293 | In Stock | |
50 mg | $442 | In Stock | |
100 mg | $592 | In Stock | |
200 mg | $783 | In Stock | |
1 mL x 10 mM (in DMSO) | $107 | In Stock |
Description | 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. |
Targets&IC50 | BTK:0.3 nM (Kd), BTK:1 nM (IC50) |
In vitro | BIIB068 inhibits B cell, neutrophil and monocyte activation in vitro, but not T cell responses. |
In vivo | 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. |
Molecular Weight | 435.52 |
Formula | C23H29N7O2 |
Cas No. | 1798787-27-5 |
Smiles | CC(C)OC1CN(C1)C(=O)NCc1ccc(cc1C)-c1ccnc(Nc2cnn(C)c2)n1 |
Relative Density. | 1.30 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (68.88 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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