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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-BIIB091
BIIB091

Chemical Structure : BIIB091

CAS No.: 2247614-80-6

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BIIB091 (BIIB 091)

货号: PC-72229Not For Human Use, Lab Use Only.

BIIB091 (BIIB 091) is a novel potent, selective, reversible BTK inhibitor with IC50 of 0.45 nM in enzymatic assays.

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2 mg ￥3980 In stock
5 mg ￥5980 In stock
10 mg ￥9580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BIIB091 (BIIB 091) is a novel potent, selective, reversible BTK inhibitor with IC50 of 0.45 nM in enzymatic assays.
BIIB091 demonstrated > 500-fold selectivity for BTK relative to all other kinases from a panel of >400 individual kinases evaluated in the DiscoverX KINOMEscan.
BIIB091 inhibited CD69 induction in anti-BCR-stimulated B cells in a dose‐dependent manner in PBMCs (IC50=5.4 nM) and in mouse splenocytes (IC50=16 nM).
BIIB091 blocks B‐cell proliferation and antigen-presenting functions in vitro and the associated B‐cell activation transcriptional programme, effectively blocks BCR-mediated antigen presentation to T cells and blocks myeloid cell functions in vitro.
BIIB091 blocks B-cell activation and differentiation into antibody-secreting and germinal center B cells in vivo, also demonstrates complete inhibition of B-cell activation over the dosing interval in a human phase 1 trial.

物理化学性质&存储条件

分子量 541.66
分子式 C29H35N9O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO (5.4 mg/mL)
Chemical Name/SMILES

1H-1,2,3-Triazole-4-carboxamide, 1-(1,1-dimethylethyl)-N-[(5R)-2,3,4,5-tetrahydro-8-[2-[(1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-2-(3-oxetanyl)-1H-2-benzazepin-5-yl]

参考文献

1. Hopkins BT, et al. J Med Chem. 2022 Jan 27;65(2):1206-1224.

2. Bame E, et al. Clin Transl Immunology. 2021 Jun 14;10(6):e1295.

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