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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-BIIB129
BIIB129

Chemical Structure : BIIB129

CAS No.: 2770960-52-4

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BIIB129 (BIIB-129)

货号: PC-22306Not For Human Use, Lab Use Only.

BIIB129 (BIIB-129) is a potent, selective, brain-penetrant and covalent inhibitor of BTK with binding KD of 0.63 nM, covently targets side chain nitrogen of Asn484 in BTK.

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10 mg ￥2180 In stock
25 mg ￥3680 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

BIIB129 (BIIB-129) is a potent, selective, brain-penetrant and covalent inhibitor of BTK with binding KD of 0.63 nM, covently targets side chain nitrogen of Asn484 in BTK.
BIIB129 inhibits CD69 expression on CD19+ B cells in human whole blood upon stimulation with anti-IgD with IC50 of 79 nM.
BIIB129 potently inhibits TMD8 B cell proliferation with IC50 of 0.82 nM.
BIIB129 has high selectivity scores (S(10)-score = 0.025 in a selectivity panel of 403 kinases.
BIIB129 has sufficient bioavailability in rats and cyno, and PKPB modeling suggested low projected total human doses to cover the IC90 in the brain over the dosing interval (20 and 40 mg BID, respectively).
BIIB129 demonstrates BTK-dependent in vivo efficacy in the CNS in two distinct preclinical models by inhibiting both TMD8 B cells transplanted in the CNS of immunodeficient mice and microglial activity in an anti-MOG mouse model.

物理化学性质&存储条件

分子量 366.43
分子式 C19H22N6O2
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
Chemical Name/SMILES

N-Methyl-N-((1s,3s)-3-methyl-3-((6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)oxy)cyclobutyl)acrylamide

参考文献

1. Himmelbauer MK, et al. J Med Chem. 2024 May 7. doi: 10.1021/acs.jmedchem.4c00220.

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