BGB-102

BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC₅₀s of 9.6 nM, 18 nM and 40.3 nM, respectively. IC50 & Target: IC50: 9.6 nM (EGFR), 18 nM (HER2), 40.3 nM (HER4)^[1] In Vitro: JNJ-26483327 (5 µM or 10 µM) with Herceptin treatment decreases HER2 phosphorylation in SKBR3 cells. JNJ-26483327 exerts greater inhibition of cell viability after 3, 6, or 8 d of treatment compared to Herceptin or JNJ-26483327 alone. JNJ-26483327 with TAPI-1 exerts less cell viability inhibition than Herceptin alone in both SKBR3 and BT474 cells^[1]. In Vivo: JNJ-26483327 (75 mg/kg, p.o.) delays xenograft tumour growth compared to vehicle treatment, but when combines with Herceptin, they can abrogate the PKB feedback loop and is synergistic in inhibition of xenograft tumour growth^[1].