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首页-小分子抑制剂&激动剂-Tyrosine Kinase-VEGFR-T-1840383
T-1840383

Chemical Structure : T-1840383

CAS No.: 1195779-24-8

T-1840383 (T1840383)

货号: PC-63356Not For Human Use, Lab Use Only.

T-1840383 is a potent, ATP-competitive, dual c-Met/VEGFR-2 inhibitor with IC50 of 1.9, 7.7, 2.2 and 5.5 nM for c-Met, VEGFR1, 2 and 3, respectively.

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

    生物&药学活性

    T-1840383 is a potent, ATP-competitive, dual c-Met/VEGFR-2 inhibitor with IC50 of 1.9, 7.7, 2.2 and 5.5 nM for c-Met, VEGFR1, 2 and 3, respectively.
    T-1840383 also potently inhibit several kinases including c-Mer, Ret, Ron, Rse, Tie-2, and TrkA as well as mutants of Abl, c-Kit, FGFR2, and PDGFRα with IC50 of <10 nM.
    T-1840383 inhibits HGF-stimulated c-Met phosphorylation (IC50=8.8 nM) in A549 cells, inhibits c-Met–dependent cell proliferation in vitro, inhibits VEGF receptor-2 phosphorylation and VEGF signaling in HUVECs.
    T-1840383 shows potent antitumor efficacy in a wide variety of human tumor xenograft mouse models, along with reduction of c-Met phosphorylation levels and microvessel density within tumor xenografts.

    物理化学性质&存储条件

    分子量 574.009
    分子式 C30H25ClFN5O4
    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-[4-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-a]pyridin-6-yl}oxy)-3-fluorophenyl]-6-methyl-2-oxo-1-phenyl-1,2-dihydropyridine-3-carboxamide hydrochloride

    参考文献

    1. Awazu Y, et al. Mol Cancer Ther. 2013 Jun;12(6):913-24.

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