BGB-102 is a potent multi-kinase inhibitor against HER2, EGFR, and HER4 (IC50s: 18 nM, 9.6 nM, and 40.3 nM).

BGB-102 (JNJ-26483327; 5 μM or 10 μM) with Herceptin treatment decreases HER2 phosphorylation in SKBR3 cells. JNJ-26483327 with TAPI-1 exerts less cell viability inhibition than Herceptin alone in both SKBR3 and BT474 cells. JNJ-26483327 exerts greater inhibition of cell viability after 3, 6, or 8 d of treatment compared to Herceptin or JNJ-26483327 alone.

Compared to vehicle treatment, JNJ-26483327 (75 mg/kg, p.o.) delays xenograft tumor growth, but when combines with Herceptin, they can abrogate the PKB feedback loop and is synergistic in inhibition of xenograft tumor growth.

807640-87-5

C22H25BrN4O2

457.36

JNJ-26483327

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years