tcsc1605 WHI-P154

WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC₅₀s of 4 nM and 1.8 μM, respectively.

IC50 & Target: IC50: 4 nM (EGFR), 1.8 μM (JAK3)^[1]

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].