| 货号 | 13032-1mg |
| 描述 | The fibroblast growth factor receptors (FGFRs) are cell surface receptors with intrinsic tyrosine kinase activity, which is necessary for receptor activation and signal propagation. PD 173074 is a potent and selective inhibitor of FGFR tyrosine kinase activity, blocking autophosphorylation of FGFR1 with an IC50 value of 21.5 nM.1 For comparison, it weakly inhibits PDGFR and c-Src (IC50 = 17.6 and 19.8 μM, respectively) and has no effect on EGFR, InsR, MEK, or PKC.1 PD 173074 also prevents signaling, at nanomolar levels, through FGFR2-5.2,3,4,5,6 Inhibition of FGFR signaling using PD 173074, impairs angiogenesis5,2 as well as self-renewal of stem cells via ERK1/2 activation.7,8,6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Mohammadi, M.,Froum, S.,Hamby, J.M., et al. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO Journal 17(20), 5896-5904 (1998). 2.Skaper, S.D.,Kee, W.J.,Facci, L., et al. The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. Journal of Neurochemistry 75, 1520-1527 (2000). 3.Koziczak, M.,Holbro, T., and Hynes, N.E. Blocking of FGFR signaling inhibits breast cancer cell proliferation through downregulation of D-type cyclins. Oncogene 23, 3501-3508 (2004). 4.Grand, E.K.,Chase, A.J.,Heath, C., et al. Targeting FGFR3 in multiple myeloma: inhibition of t(4;14)-positive cells by SU5402 and PD173074. Leukemia 18, 962-966 (2004). 5.St.Bernard, R.,Zheng, L.,Liu, W., et al. Fibroblast growth factor receptors as molecular targets in thyroid carcinoma. Endocrinology 146(3), 1145-1153 (2005). 6.Stavridis, M.P.,Lunn, J.S.,Collins, B.J., et al. A discrete period of FGF-induced Erk1/2 signalling is required for vertebrate neural specification. Development 134, 2889-2894 (2007). 7.Kunath, T.,Saba-El-Leil, M.K.,Almousailleakh, M., et al. FGF stimulation of the Erk1/2 signalling cascade triggers transition of pluripotent embryonic stem cells from self-renewal to lineage commitment. Development 134, 2895-2902 (2007). 8.Zaragosi, L.E.,Ailhaud, G., and Dani, C. Autocrine fibroblast growth factor 2 signaling is critical for self-renewal of human multipotent adipose-derived stem cells. Stem Cells 24, 2412-2419 (2006). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 523.7 |
| 分子式 | C28H41N7O3 |
| CAS号 | 219580-11-7 |
| 稳定性 | ≥ 2 years |
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