Encorafenib (LGX818)

Bezeichnung:Encorafenib (LGX818)

CAS-Nr1269440-17-6

Englisch Name:Encorafenib (LGX818)

CBNumberCB42668617

SummenformelC22H27ClFN7O4S

Molgewicht540.01

MOL-Datei1269440-17-6.mol

Encorafenib (LGX818) physikalisch-chemischer Eigenschaften

Schmelzpunkt	184-185°C
Dichte	1.45±0.1 g/cm3(Predicted)
storage temp.	-20°C Freezer, Under inert atmosphere
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
pka	5.94±0.10(Predicted)
Aggregatzustand	Solid
Farbe	White to Off-White

Gefahreninformationscode (GHS)

Encorafenib (LGX818) Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Encorafenib (LGX818) is a new-generation BRAF inhibitor that is under evaluation in clinical trials. However, the underlying mechanism remains to be elucidated. Here we show that LGX818 potently decreased ERK phosphorylation and inhibited proliferation in BRAFV600E melanoma cell lines. Moreover, LGX818 downregulated CyclinD1 in a glycogen synthase kinase 3β-independent manner and induced cell cycle arrest in the G1 phase.
Verwenden
LGX 818 is potent and selective BRAFV600E kinase inhibitor and can be used for the treatment of proliferative diseases such as solid tumor diseases.
Trademarks
Braftovi
Allgemeine Beschreibung
Class: dual threonine/tyrosine kinase; Treatment: melanoma with BRAFV600E/K; Oral bioavailability = 85%; Elimination half-life = 6 h; Protein binding = 86%
Biologische Aktivität
Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM. Phase 3.
Pharmakokinetik
Encorafenib shows an oral bioavailability of 85% and a half-life of 6 h. It is administered orally once a day (450 mg), whereas the other two dabrafenib and vemurafenib are taken twice a day (Table 2, Section 10.1). The primary metabolic pathway is N-dealkylation, with CYP3A4 as the main contributor (Fig. 1).
Clinical Use
Encorafenib (LGX818) is a new-generation BRAF inhibitor. It is currently under investigation in clinical trials for the treatment of BRAF mutant metastatic melanoma patients . LGX818 induces sustained mitogen-activated protein kinase (MAPK) pathway inhibition and has selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E. However, the mechanism by which LGX818 suppresses BRAF mutant melanoma cell proliferation has not been thoroughly investigated.
target
B-RAF(V600E)
Einzelnachweise
[1] stuart d d, li n, poon d j, et al. preclinical profile of lgx818: a potent and selective raf kinase inhibitor. cancer research, 2012, 72(8 supplement): 3790.
[2] huang t, karsy m, zhuge j, et al. b-raf and the inhibitors: from bench to bedside. j hematol oncol, 2013, 6(1): 30.

Encorafenib (LGX818) Upstream-Materialien And Downstream Produkte

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