PD153035(ZM 252868, AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM. PD153035 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.PD153035 induces a dose-dependent growth inhibition in nasopharyngeal carcinoma (NPC) cells including NPC-TW01, NPC-TW04, and HONE1 cell lines with IC50 of 12.9 μM, 9.8 μM and 18.6μM, respectively. PD153035 inhibits other purified tyrosine kinases only at micromolar or higher concentrations.
|Source||Chem Biol Interact (2016). Figure 6. PD153035|
|Incubation Time||72 h|
|Results||To address this question, we measured DNA synthesis using EdU labeling in cells treated for 72 h with TCDD in the presence or absence of the EGFR inhibitor PD153035 (300 nM). Compared to basal cells, TCDD treatment significantly increased the percentage of the cell population that was proliferating|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Inhibitors of epidermoid growth factor receptor suppress cell growth and enhance chemosensitivity of nasopharyngeal cancer cells in vitro.
Hsu CH, et al. Oncology. 2005;68(4-6):538-47. PMID: 16037687.
Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor.
Bridges AJ, et al. J Med Chem. 1996 Jan 5;39(1):267-76. PMID: 8568816.
A specific inhibitor of the epidermal growth factor receptor tyrosine kinase.
Fry DW, et al. Science. 1994 Aug 19;265(5175):1093-5. PMID: 8066447.
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