PD153035 hydrochloride (ZM 252868, AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM. PD153035 HCl 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. PD 153035 inhibits other purified tyrosine kinases only at micromolar or higher concentrations.
|Cell lines||A431, Difi, DU145, MDA-MB-468 and ME180|
|Preparation method||Seeding cells in sixwell plates. The next day, changing cells to medium containing 0.5% FBS for 18 hours, and then adding PD153035 at various concentrations to the cultures. After 72 hours of treatment, washing cells once with PBS, harvesting with 0.1% human trypsin-l mM EDTA in PBS, and counting with a Coulter counter. The CMK cells grow in suspension and, therefore, do not require trypsinization.|
|Incubation time||72 hours|
|Animal models||A431 cells are injected into the outbred nude mice|
|Formulation||PD153035 is dissolved in water.|
|Administration||Administered via i.p.|
|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.
|Solubility||DMSO <1 mg/mL
Water <1 mg/mL
Ethanol <1 mg/mL
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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