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CAS No. : 2247614-80-6
MCE 国际站:BIIB091
产品活性:BIIB091 是一种有效,选择性,具有口服活性和可逆的 BTK 抑制剂,IC50 值 <0.5 nM。BIIB091 与 BTK 蛋白结合,将 Tyr-551 隔离成具有出色亲和力的非活性构象。 BIIB091 可用于多发性硬化症的研究。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:Btk
In Vitro: BIIB091 inhibits the phosphorylation of PLCγ2 in the Ramos human B-cell line, with an IC50 of 6.9 nM.
BIIB091 blocks anti-IgM-stimulated CD69 activation in PBMCs with an IC50 of 6.9 nM.
BIIB091 inhibits FcγR-induced ROS production in purified primary neutrophils, with an IC50 of 4.5 nM.
BIIB091 inhibits FcγRI and FcγRIII-mediated TNFα secretion upon simulation with FcγR agonists such as coated human IgG (all FcγR, IC50=5.6 nM), anti-CD16 (FcγRIII, IC50=8.0 nM), anti-CD64 (FcγRI IC50=3.1 nM), and cross-linked anti-CD16 (FcγRIII IC50=1.3 nM) in human monocytes.
BIIB091 inhibits the phosphorylation of BTK (IC50=24 nM) and blocks both BCR mediated B cell and FcεR-induced basophil activation as measured by inhibition of CD69 and CD63 expression (IC50=71 nM and IC50=82 nM, respectively) in the whole blood assays.
In Vivo: BIIB091 (0.03-30 mg/kg; p.o. twice daily for 10 d) reduces the anti-NP IgM antibody titers (88%, 77%, 59%, 59%, 44%, 34%, and 22%) in the TI-2 immunization model.
Pharmacokinetics of BIIB091 in preclinical species
species |
IV (1 mg/kg) |
PO (5 mg/kg) in HMPC/Tween |
T1/2 (h) |
AUCinf (h•ng/mL) |
CL (mL/min/kg) |
CL %QH |
Vdss (L/kg) |
Tmax (h) |
Cmax (ng/mL) |
AUCinf (h•ng/mL) |
%F |
rat |
2.1 |
748 |
10 |
22 |
0.4 |
0.9 |
693 |
1522 |
42 |
cyno |
1.1 |
943 |
18 |
44 |
0.7 |
0.33 |
1104 |
1446 |
31 |
dog |
6.0 |
1675 |
12 |
33 |
1.7 |
1.6 |
1440 |
6075 |
89 |
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