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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Trk Receptor-Utatrectinib
Utatrectinib

Chemical Structure : Utatrectinib

CAS No.: 1079274-94-4

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Utatrectinib (AZD7451, AZ12607092)

货号: PC-73452Not For Human Use, Lab Use Only.

Utatrectinib (AZD7451, AZ12607092) is a potent, selective, small molecule pan-Trk (NTRK) inhibitor with IC50 of 0.2-3.0 nM against TrkA, TrkB, and TrkC.

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

    生物&药学活性

    Utatrectinib (AZD7451, AZ12607092) is a potent, selective, small molecule pan-Trk (NTRK) inhibitor with IC50 of 0.2-3.0 nM against TrkA, TrkB, and TrkC.
    Binding of AZD7451 to TrkA, TrkB, and TrkC would be expected to inhibit responses associated with NGF, BDNF, and NT3, respectively.
    AZD7451 completely blocked TrkC activation and associated tumorigenic behaviors at sub-micromolar concentrations in normal salivary gland tissue.
    AZD7451 showed efficacy and low toxicity in pre-clinical studies on adenoid cystic carcinoma (ACC) tumors engrafted in mice.
    AZD7451 potently inhibited in vitro growth and proliferation of the KM12 cell line harboring the NTRK1-fusion at 2 nM, AZD7451 inhibited proliferation of H460 cells at 5 nM, with TRKA phosphorylation inhibition.

    物理化学性质&存储条件

    分子量 382.403
    分子式 C18H19FN8O
    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-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-3-(5-isopropoxy-1H-pyrazol-3-yl)-3H-imidazo[4,5-b]pyridin-5-amine

    参考文献

    1. Ivanov SV, et al. Oncogene. 2013 Aug 8;32(32):3698-710.

    2. Tatematsu T, et al. Mol Clin Oncol. 2014 Sep;2(5):725-730.

    3. Li H, et al. J Cancer. 2019 Oct 15;10(24):6065-6073.

    4. Tao Wang, et al. J Med Chem. 2008 Aug 14;51(15):4672-84.

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