LGX 818

Modify Date: 2024-01-02 19:53:14

LGX 818 Structure
LGX 818 structure
Common Name LGX 818
CAS Number 1269440-17-6 Molecular Weight 540.011
Density 1.5±0.1 g/cm3 Boiling Point N/A
Molecular Formula C22H27ClFN7O4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of LGX 818


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

 Names

Name methyl N-[(2S)-1-[[4-[3-[5-chloro-2-fluoro-3-(methanesulfonamido)phenyl]-1-propan-2-ylpyrazol-4-yl]pyrimidin-2-yl]amino]propan-2-yl]carbamate
Synonym More Synonyms

 LGX 818 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
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.

 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)

 Synonyms

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