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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FLT3-NCGC1481
NCGC1481

Chemical Structure : NCGC1481

CAS No.: 2193085-94-6

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NCGC1481 (NCGC 1481)

货号: PC-72044Not For Human Use, Lab Use Only.

NCGC1481 (NCGC 1481) is a novel potent, type I kinase inhibitor against IRAK1/4 and FLT3, with IC50 of 22.6/0.8 nM and <0.5 nM respectively.

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

    生物&药学活性

    NCGC1481 (NCGC 1481) is a novel potent, type I kinase inhibitor against IRAK1/4 and FLT3, with IC50 of 22.6/0.8 nM and <0.5 nM respectively.
    NCGC1481 exhibited potent binding affinity for IRAK1 (Kd=2.9 nM), IRAK4 (Kd=0.3 nM), and FLT3 (Kd=0.3 nM), NCGC1481 demonstrated modest selectivity (>10-fold selectivity versus more than 80% of tested kinases relative to IRAK1, IRAK4, and FLT3) against 369 kinases, inhibited 12/259 kinases with IC50 of <250 nM in the KiNativ in situ kinase profiling platform.
    NCGC1481 inhibits compensatory IRAK1/4 signaling and prevents adaptive resistance in FLT3-ITD AML cells in vitro and in vivo, NCGC1481 effectively targets resistant FLT3-ITD AML xenografts.
    NCGC1481 targets clinically relevant FLT3-mutant AML cells in vitro.
    NCGC1481 is a potent and efficacious small-molecule inhibitor of FLT3-ITD and clinically relevant mutants (D835Y Kd=0.29 nM).
    NCGC1481 exhibited superior antileukemic activity against the common, clinically relevant FLT3-mutant AML cells in vitro and in vivo.

    物理化学性质&存储条件

    分子量 389.463
    分子式 C21H23N7O
    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

    6-(7-Methoxy-6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl)-N-(pyrrolidin-3-yl)pyridin-2-amine

    参考文献

    1. Jones LM, et al. J Clin Invest. 2020 Apr 1;130(4):2017-2023.

    2. Sci Transl Med. 2019 Sep 4;11(508):eaaw8828.

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