PD153035 HCl

2 years -80 in solvent

Administered via i.p.

A431, Difi, DU145, MDA-MB-468 and ME180

<=80 mg/kg

5.2 pM (Ki), 5.2 pM (Ki), 5.2 pM (Ki), 5.2 pM (Ki), 5.2 pM (Ki), 5.2 pM (Ki)

In A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035 at 80 mg/kg inhibit EGF receptor tyrosine kinase activity. [5] PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice. [6] Pretreatment of EGFR inhibitors by 24 hours significantly enhances the cytotoxic effect of doxorubicin, paclitaxel, cisplatin, and 5-fluororuacil in NPCTW04 cells. [3]

Inhibition of EGF receptor tyrosine kinase, Enzyme reactions are performed in a total volume of 0.1 mL containing 25 mM Hepes (pH 7.4), 5 mM MgCl2, 2 mM MnCl2, 50 uM sodium vanadate, 0.5 to 1.0 ng of enzyme (which also contains enough EGF to make the final concentrations 2 ug/mL), 10 uM ATP containing 1 uCi of [32P]ATP, varying concentrations of PD153035, and 200 uM of a substrate peptide based on a portion of phospholipase C-gammal having the sequence Lys-His-Lys-Lys-Leu-Ala-Glu-Gly-Ser-Ala-Tyr472-Glu-Glu-Val. The reaction is initiated by the addition of ATP. After 10 minutes at room temperature, the reaction is terminated by addition of 2 mL of 75 mM phosphoric acid, and the solution is passed through a 2.5-cm phosphocellulose filter disk that binds the peptide. The filter is washed five times with 75 mM phosphoric acid and placed in a vial with 5 mL of scintillation fluid. The uninhibited control activity produces approximately 100, 000 cpm.

DMSO 0.5 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL

N-(3-bromophenyl)-6, 7-dimethoxyquinazolin-4-amine hydrochloride