Biological Activity
WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.
In Vitro
WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively[1]. WHI-P154 significantly enhances the sensitivity of ABCG2-overexpressing cells to its substrates. WHI-P154 (4 μM) moderately sensitizes ABCB1-overexpressing KB-C2 cells to its substrates whereas shows no sensitizing effect on ABCC1-, ABCC2 or ABCC10-mediated drug resistance. Moreover, WHI-P154 (4 μM) causes a significant increase in the intracellular accumulation of [3H]-mitoxantrone in ABCG2-overexpressing cells. WHI-P154 alters the expression levels rather than the localization of the ABCG2 protein in ABCG2-overexpressing cells[2].
In Vivo
No in vivo data are provided in the current product source. Contact us for further information.
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.