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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Checkpoint Kinase (Chk)-BEN-28010
BEN-28010

Chemical Structure : BEN-28010

CAS No.: 3033961-38-2

BEN-28010 (BEN28010)

货号: PC-24518Not For Human Use, Lab Use Only.

BEN-28010 is a potent selective, orally bioavailable and brain-penetrant checkpoint kinase 1 (CHK1) inhibitor with IC50 of 4 nM, 450-fold selective over CHK2.

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

    生物&药学活性

    BEN-28010 is a potent selective, orally bioavailable and brain-penetrant checkpoint kinase 1 (CHK1) inhibitor with IC50 of 4 nM, 450-fold selective over CHK2.
    BEN-28010 potently inhibits pCHK1 in SW620 cells with IC50 of 0.45 uM, inhibits LN-18/A172 cell viability with IC50 of 0.14/3.3 uM.
    BEN-28010 also has good selectivity for CHK1 over the diverse Cerep SafetyScreen87 panel of 87 enzymes.
    BEN-28010 demonstrated efficacy in several GBM CDX and PDX models as a monotherapy and in combination with ionizing radiation, including improved overall survival in an intracranially implanted GBM PDX mouse model.

    物理化学性质&存储条件

    分子量 374.45
    分子式 C20H22N8
    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

    (R)-5-((1-(4-(3-(Dimethylamino)pyrrolidin-1-yl)phenyl)-1H-imidazol-4-yl) amino)pyrazine-2-carbonitrile

    参考文献

    1. Rawling MJ, et al. J Med Chem. 2025 Apr 24. doi: 10.1021/acs.jmedchem.5c00279.

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