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Nek2 inhibitor (R)-21

Chemical Structure : Nek2 inhibitor (R)-21

CAS No.: 1364269-10-2

Nek2 inhibitor (R)-21

货号: PC-61483Not For Human Use, Lab Use Only.

A potent and selective NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 22 nM, >200-fold selectivity over Plk1, Mps1, Aurora A and CDK2.

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

    生物&药学活性

    Nek2 inhibitor (R)-21 is a potent and selective NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 22 nM, >200-fold selectivity over Plk1, Mps1, Aurora A and CDK2.
    Nek2 inhibitor (R)-21 also shows >100-fold selectivity over a panel of 24 kinases.
    Nek2 inhibitor (R)-21 down-regulates C-Nap1 phosphoryation with IC50 of 0.8 uM, shows antiproliferative effect on U2OS, MDA-MB-231, HeLa and MCF7 cell with GI50 of 1.82, 4.16, 0.59 and 2.17 uM, respectively.
    Nek2 inhibitor (R)-21 is a valuable tool for investigating the role of Nek2 in the cell cycle and its function in mitotic organization.

    物理化学性质&存储条件

    分子量 490.545
    分子式 C24H25F3N4O2S
    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)-(Z)-4-(2-Amino-5-(4-((dimethylamino)methyl)thiophen-2-yl)pyridin-3-yl)-2-((5,5,5-trifluoropent-3-en-2-yl)oxy)benzamide

    参考文献

    1. Innocenti P, et al. J Med Chem. 2012 Apr 12;55(7):3228-41.

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