SU4984 是一种蛋白质酪氨酸激酶抑制剂，抑制成纤维细胞生长因子受体 1 (FGFR1) 的 IC50 值为 10-20 μM。SU4984 还可抑制血小板衍生的生长因子受体和胰岛素受体的活性。SU4984 可用于癌症研究。
SU4984 is a protein tyrosine kinase inhibitor, with an IC50 of 10-20 μM for fibroblast growth factor receptor 1 (FGFR1). SU4984 is also inhibits platelet-derived growth factor receptor, and insulin receptor. SU4984 can be used for the research of cancer[1][2][3].
SU4984 (5-100 μM; 5 min) inhibits the kinase activity of FGFR1K with an IC50 of 10-20 μM in the presence of 1 mM adenosine triphosphate (ATP)[1].SU4984 (10-90 μM; 5 min) inhibits the autophosphorylation of FGFR1 induced by aFGF in NIH 3T3 cells, with an IC50 of 20-40 μM[1].SU4984 (5 μM) substantially reduces tyrosine phosphorylation of the wild-type receptor and reduces 50% phosphorylation of constitutive C2 KIT[2].SU4984 (1-10 μM; 6 days) kills the C2 and P815 cells[2].
参考文献:
[1]. Mohammadi M, et, al. Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors. Science. 1997 May 9;276(5314):955-60.
[2]. Ma Y, et, al. Indolinone derivatives inhibit constitutively activated KIT mutants and kill neoplastic mast cells. J Invest Dermatol. 2000 Feb;114(2):392-4.
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