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Gandotinib

CAS No. : 1229236-86-5

MCE 站：Gandotinib

产品活性：Gandotinib (LY2784544) 是一种有效的 JAK2 抑制剂，IC₅₀ 为 3 nM。Gandotinib (LY2784544) 也抑制FLT3，FLT4，FGFR2，TYK2 和 TRKB，IC₅₀ 分别为 4，25，32，44 和 95 nM。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：JAK  |  FLT3  |  FGFR  |  VEGFR

In Vitro: Gandotinib (LY2784544), a potent, selective and ATP-competitive inhibitor of janus kinase 2 (JAK2) tyrosine kinase. LY2784544 effectively inhibits JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC₅₀=20 and 55 nM, respectively). In comparison, Gandotinib (LY2784544) is much less potent at inhibiting interleukin-3-stimulated wild-type JAK2-mediated signaling and cell proliferation (IC₅₀=1183 and 1309 nM, respectively). Gandotinib (LY2784544) potently inhibits the JAK2V617F signaling (IC₅₀=20 nM) but, remarkably, shows very minimal activity against the IL-3-activated wild-type JAK2 signaling with an IC₅₀ of 1183 nM. LY2784544 inhibits the proliferation of JAK2V617F-expressing cells (IC₅₀=55 nM) and is markedly less potent as an inhibitor of the proliferation of IL-3-stimulated wild-type JAK2 expressing Ba/F3 cells (IC₅₀=1309 nM). Gandotinib (LY2784544) is potent in the cell-based TF-1 JAK2 assay (IC₅₀=45 nM) and had the desired threshold selectivity in the NK-92 JAK3/JAK1 heterodimer assay (942 nM).

In Vivo: Gandotinib (LY2784544) effectively inhibits STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP (green fluorescent protein) ascitic tumor cells (TED₅₀=12.7 mg/kg) and significantly reduces (P<0.05) Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model (TED₅₀=13.7 mg/kg, twice daily).

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