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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-JNJ-64264681
JNJ-64264681

Chemical Structure : JNJ-64264681

CAS No.: 2101524-34-7

JNJ-64264681 (JNJ 64264681)

货号: PC-49425Not For Human Use, Lab Use Only.

JNJ-64264681 is a potent, selective, covalent, irreversible BTK inhibitor with Ki of 48.5 nM, enzymatic IC50 of 558 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    JNJ-64264681 is a potent, selective, covalent, irreversible BTK inhibitor with Ki of 48.5 nM, enzymatic IC50 of 558 nM.
    has IC50 of 99 nM in mouse CD69 splenocyte assay triggering B-cell activation by anti-IgM stimulation.
    JNJ-64264681 targets BTK Cys481 with IC50 of 21 nM in enzyme-linked immunosorbent assay.
    JNJ-64264681 shows antiproliferative activity (IC50<100 nM) against a panel of ABC-DLBCL cell lines─OCI-Ly3, OCI-Ly10, TMD8, and HBL-1, and CD79b mutant ABC-DLBCL cell lines (OCI-Ly10, TMD8, and HBL-1).
    JNJ-64264681 (10, 30, and 100 mg/kg administered QD) inhibited tumor growth by 24%, 35%, and 51% TGI (30, 45, and 65% ΔTGI), respectively, in OCI-Ly10 human DLBCL xenografts in NSG mice.

    物理化学性质&存储条件

    分子量 518.636
    分子式 C27H30N6O3S
    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-((1R,2S)-2-acrylamidocyclopentyl)-5-(6-isobutyl-4-methylpyridin-3-yl)-4-oxo-4,5-dihydro-3H-1-thia-3,5,8-triazaacenaphthylene-2-carboxamide

    参考文献

    1. Tichenor MS, et al. J Med Chem. 2022 Nov 10;65(21):14326-14336.

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