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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 Experiment | |
|---|---|
| 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. |
| Concentrations | 0-3 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | A431 cells are injected into the outbred nude mice |
| Formulation | PD153035 is dissolved in water. |
| Dosages | ≤80 mg/kg |
| Administration | Administered via i.p. |
| Molecular Weight | 396.67 |
| Formula | C16H14BrN3O2.HCl |
| CAS Number | 183322-45-4 |
| Solubility (25°C) | DMSO 4 mg/mL (Need ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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