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LGX 818

Names

[ CAS No. ]:
1269440-17-6

[ Name ]:
LGX 818

[Synonym ]:
LGX-818
Encorafenib
NVP-LGX818-NXA
LGX818
Encorafenib (LGX818)
methyl N-[(2S)-1-({4-[3-(5-chloro-2-fluoro-3-methanesulfonamidophenyl)-1-(propan-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl}amino)propan-2-yl]carbamate
T6N CNJ BM1Y1&MVO1& D- DT5NNJ AY1&1 CR CG FF EMSW1 &&S Form
UNII-8L7891MRB6
Carbamic acid, N-[(1S)-2-[[4-[3-[5-chloro-2-fluoro-3-[(methylsulfonyl)amino]phenyl]-1-(1-methylethyl)-1H-pyrazol-4-yl]-2-pyrimidinyl]amino]-1-methylethyl]-, methyl ester
(S)-methyl (1-((4-(3-(5-chloro-2-fluoro-3-(methylsulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-yl)carbamate
Methyl [(2S)-1-{[4-(3-{5-chloro-2-fluoro-3-[(methylsulfonyl)amino]phenyl}-1-isopropyl-1H-pyrazol-4-yl)-2-pyrimidinyl]amino}-2-propanyl]carbamate

Biological Activity

[Description]:

Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).

[Related Catalog]:

Signaling Pathways >> MAPK/ERK Pathway >> Raf
Research Areas >> Cancer

[Target]

IC50: 0.3 nM (BRafV600E)


[In Vitro]

Encorafenib (LGX818) is a potent drug that can prevents diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf[1]. Encorafenib (LGX818) (10 nM) suppresses the ERK/MAPK pathway and displays marked inhibition of pERK in A375, G361 and SK-MEL-24 cells. 10 nM Encorafenib (LGX818) treatment for 12 days potently inhibits colony formation in A375, G361 and SK-MEL-24 cells, but not in RPMI7951 and C8161 cells. Encorafenib (LGX818) treatment induces a steady increase in the β-catenin level in G361 cells over time[2].

[References]

[1]. Compounds and compositions as protein kinase inhibitors. Patent WO 2011025927 A1

[2]. Li Z, et al. Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells. Cancer Lett. 2016 Jan 28;370(2):332-44.


[Related Small Molecules]

PLX8394 | Doramapimod (BIRB 796) | PLX-4720 | LY 3009120 | GW5074 | RAF265 (CHIR-265) | AZ 628 | RAF709 | CEP-32496 | GDC-0879 | LXH254 | TAK-632 | PLX7904 | HG6-64-1 | RO 5126766

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C22H27ClFN7O4S

[ Molecular Weight ]:
540.011

[ Exact Mass ]:
539.151794

[ PSA ]:
152.00000

[ LogP ]:
2.56

[ Index of Refraction ]:
1.641

[ Storage condition ]:
-20℃

[ Water Solubility ]:
Insuluble (7.0E-4 g/L) (25 ºC)

Related Compounds