货号 | 3044/50 |
别名 | N-[2-[[4-(Diethylamino)butyl]amino] |
供应商 | Tocris |
生物活性 | Selective FGFR1 and FGFR3 inhibitor (IC50 values are 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively, and > 50000 nM for EGFR, InsR, MEK and PKC). Inhibits VEGF- and FGF-induced angiogenesis in the mouse cornea model of angiogenesis. Inhibits proliferation and differentiation of oligodendrocyte progenitors. Suppresses cell proliferation in cell lines expressing mutated FGFR3 protein. Blocks tumor growth in H510 and H69 SCLC xenograft models. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 523.67 |
分子式 | C28H41N7O3 |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
CAS号 | 219580-11-7 |
参考文献 | Miyakeet al (2010) 1-tert-butyl-3-[6-(3,5-dimethoxy-phenyl)-2-(4-diethylamino-butylamino)-pyrido[2,3-d]pyrimidin-7-yl]-urea (PD173074), a selective tyrosine kinase inhibitor of fibroblast growth factor receptor-3 (FGFR3), inhibits cell proliferation of bladder cancer carrying the FGFR3 gene mutation along with up-regulation of p27/Kip1 and G1/G0 arrest. J.Pharmacol.Exp.Ther. 332 795. PMID: 19955487. Pardoet al (2010) The fibroblast growth factor receptor inhibitor PD173074 blocks small cell lung cancer growth in vitroandin vivo. Cancer Res. 698645. Trudelet al (2004) Inhibition of fibroblast growth factor receptor 3 induces differentiation and apoptosis in t(4;14) myeloma. Neoplasia 1033521. Bansalet al (2003) 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. 74 486. PMID: 14598292. |