1269440-17-6
1269440-17-6 structure
- Name: LGX 818
- Chemical 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
- CAS Number: 1269440-17-6
- Molecular Formula: C22H27ClFN7O4S
- Molecular Weight: 540.011
- Catalog: Biochemical Inhibitor Mitogen-activated protein kinase (MAPK) Raf inhibitor
- Create Date: 2018-08-25 11:03:49
- Modify Date: 2026-06-29 22:56:45
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Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
| 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 |
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| Synonyms |
Encorafenib, 10 mM in DMSO
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 (S) - [1 - [[4 - [3 - [5-chloro-2-fluoro-3 - (methylsulfonamido) phenyl] - 1-isopropyl-1h-pyrazole-4-yl] pyrimidin-2-yl] amino] propyl-2-yl] cbamate LGX-818 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]cbamate LGX818; LGX-818; LGX 818; ENCORAFENIB (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]cbamate methyl (S)-(1-((4-(3-(5-chloro-2-fluoro-3-(methylsulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-yl)cbamate 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 Cbamic 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 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 LGX-818 Encorafenib LGX 818 (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]cbamate 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]cbamate Encorafenib (LGX818) LGX818, >= (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 NSC4820 NVP-LGX818-NXA LGX818, Encorafenib ENCORAFENIB;LGX818; LGX-818 Encorafenib (LGX818) //BP NSC-4820 LGX 818; LGX-818;LGX818 Cymoxanil Impurity 3 |
| Description | Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM). |
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| 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 |
| Density | 1.5±0.1 g/cm3 |
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| 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) |