中文名称: PD-089828
英文名称: PD-089828
CAS No: 179343-17-0
分子式: C18H18Cl2N6O
分子量: 405.28
P11586 PD-089828 ≥98% (psaitong)
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产品描述:

一种ATP竞争性FGFR-1、PDGFR-β和EGFR(IC50分别为0.15,1.76,5.47µM)抑制剂和c-Src酪氨酸激酶非竞争性抑制剂(IC50=0.18µM).也抑制MAPK,IC50值为7.1µM。PD-089828体外抑制PDGF-、EGF-和bFGF介导的酪氨酸激酶受体的自磷酸化。PD-089828具有持久的细胞活性。
PD089828 is a potent FGFR inhibitor, which inhibits human full-length fibroblast growth factor (FGF) receptor-1 (FGFR-1), platelet-derived growth factor (PDGF) receptor beta subunit (PDGFR-beta), Src nonreceptor tyrosine kinase (c-Src) and epidermal growth factor (EGF) receptor (EGFR) tyrosine kinases with half-maximal inhibitory potencies (IC50 values) of 0.15 +/- 0.02 (n = 4), 0.18 +/- 0.04 (n = 3), 1.76 +/- 0.28 (n = 4) and 5.47 +/- 0.78 (n = 6) microM, respectively. The results highlight the biological characteristics of PD 089828 as a novel, broadly active protein tyrosine kinase inhibitor with long-lasting but reversible cellular effects. The potential therapeutic use of these broadly acting, nonselective inhibitors as antiproliferative and antimigratory agents could extend to such diseases as cancer, atherosclerosis and restenosis in which redundancies in growth-signaling pathways are known to exist.

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