PD173074是一种有效的ATP竞争型的FGFR1抑制剂,对FGFR1的IC50值约为25 nM,Ki值约为40 nM。PD173074也是VEGFR2的有效抑制剂,对VEGFR2的IC50值为100-200 nM。PD173074 是一种强效的和选择性的成纤维细胞生长因子受体抑制剂(FGFR抑制剂)。成纤维细胞生长因子-2能诱导小细胞肺癌(SCLC)细胞的增殖和化疗耐药性。PD173074还能抑制FGFR1和VEGFR2的自身磷酸化,能有效阻止由FGF或VEGF诱导的血管生成,且几乎没有细胞毒性。
参考文献
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[2]. Trudel S, et al. Inhibition of fibroblast growth factor receptor 3 induces differentiation and apoptosis in t(4;14) myeloma. Blood. 2004 May 1;103(9):3521-8.
[3]. Bansal R, et al. Specific inhibitor of FGF receptor signaling: FGF-2-mediated effects on proliferation, differentiation, and MAPK activation are inhibited by PD173074 in oligodendrocyte-lineage cells. J Neurosci Res. 2003 Nov 15;74(4):486-93.
冰袋运输。粉末直接保存于-20℃,有效期3年。溶于DMSO。建议分装后-20℃避光保存,避免反复冻融。