中文名：SGI-7079
英文名：SGI-7079
纯度：≥98%
货号：S413852
Cas号：1239875-86-5
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
SGI-7079 SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.
Targets
Met ; Mer ; YES ; RET ; FLT3 16051,;
In vitro
SGI-7079 exhibits a Ki = 5.7 nM for AXL and inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed in HEK293T cells (EC50 = 100 nM). It inhibits TAM family members MER and Tyro3 similarly as AXL, and shows potent, low nM inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases. Mesenchymal cells express increased levels of the receptor tyrosine kinase Axl and show a trend toward greater sensitivity to the Axl inhibitor SGI-7079.
In vivo
SGI-7079 inhibits tumor growth in a dose-dependent manner, and at the maximum dose, inhibits tumor growth by 67%, compared with control. the combination of SGI-7079 with erlotinib reverses erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC.
Cell Research(from reference)
Cell lines：HEK-293 cells
Concentrations：0.03, 0.1, 0.3, 1, 3 μmol/L
Incubation Time：10 min
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关键字： Benzeneacetonitrile,3-?[2-?[[3-?fluoro-?4-?(4-?methyl-?1-?piperazinyl)?phenyl]?amino]?-?5-?methyl-?7H-?pyrrolo[2,?3-?d]?pyrimidin-?4-?yl]?-
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