2016年10月8日星期六

PLX7904(PB04)|paradox-breaker RAF inhibitor

PLX7904(PB04)|paradox-breaker RAF inhibitor

PLX7904(PB04) is a potent and selective paradox-breaker RAF inhibitor.

Product Name: PLX7904(PB04)|Cat No. DC9814|CAS: 1393465-84-3|Other names:PLX-7904,PLX 7907,PB04; PB-04; PB 04; paradox-breaker-04|MW: 512.14|Molecule Formular: C24H22F2N6O3S|Purity>98%

PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. PB04 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. Importantly, PB04 inhibited ERK1/2 phosphorylation in mutant BRAF melanoma cells with acquired resistance to vemurafenib/PLX4720 that is mediated by a secondary mutation in NRAS. Consistent with ERK1/2 reactivation driving the re-acquisition of malignant properties, PB04 promoted apoptosis and inhibited entry into S phase and anchorage-independent growth in mutant N-RAS-mediated vemurafenib-resistant cells.


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