BGB-102 is a potent multi-kinase inhibitor againstEGFR,HER2, andHER4withIC₅₀s of 9.6 nM, 18 nM and 40.3 nM, respectively.

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].

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].

457.36

Solid

C₂₂H₂₅BrN₄O₂

807640-87-5

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