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JAK/STAT SignalingProtein Tyrosine Kinase/RTK-
PD153035(ZM 252868; AG 1517)????????????EGFR?????????????????????Ki???IC50?????????5.2 pM???29 pM?????????PGDFR???FGFR???CSF-1???InsR???Src???????????????
EGFR
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AZD-9291-Gefitinib-Lapatinib-Afatinib-Erlotinib-AG-490-Genistein-AG-1478-Neratinib-EGF816-Olmutinib-AZD3759-Dacomitinib-Irbinitinib-CO-1686-
生物活性
Description
PD153035(ZM 252868; AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM; little effect against PGDFR, FGFR, CSF-1, InsR and Src.IC50 value: 5.2/29 pM(Ki/IC50) [1]Target: EGFRin vitro: PD 153035 shows a potent and selective inhibitory effect on tyrosine phosphorylation induced with EGF with IC50 of 15 nM and 14 nM in Swiss 3T3 fibroblast and A-431 human epidermoid carcinoma cells, respectively [1]. PD153035 shows growth inhibitory effects in cultures of EGF receptor-overexpressing human cancer cell lines including A431, Difi, DU145, MDA-MB-468 and ME180 cells with IC50 of 0.22 ??M, 0.3??M, 0.4 ??M, 0.68 ??M and 0.95 ??M, respectively [2]. in vivo: In A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035 at 80 mg/kg inhibit EGF receptor tyrosine kinase activity [3]. PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice [4].
References
[1].Fry DW, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994, 265(5175), 1093-1095.
[2].Bos M, et al. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997, 3(11), 2099-2106.
[3].Kunkel MW, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996, 13(4), 295-302.
[4].Prada PO, et al. EGFR tyrosine kinase inhibitor (PD153035) improves glucose tolerance and insulin action in high-fat diet-fed mice. Diabetes. 2009 , 58(12), 2910-2919.