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Encorafenib (LGX818)

Encorafenib (LGX818) Structure
Encorafenib (LGX818) structure
CAS No.
1269440-17-6
Chemical Name:
Encorafenib (LGX818)
Synonyms
Encorafenib;LGX818;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]carbamate;CS-1037;LGX 818;NSC4820;NSC 4820;NSC-4820;LGX818, >=98%
CBNumber:
CB42668617
Molecular Formula:
C22H27ClFN7O4S
Molecular Weight:
540.01
MDL Number:
MFCD25976758
MOL File:
1269440-17-6.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-07-23 14:48:42
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Encorafenib (LGX818) Properties

Melting point 184-185°C
Density 1.45±0.1 g/cm3(Predicted)
storage temp. -20°C Freezer, Under inert atmosphere
solubility DMSO (Slightly), Methanol (Slightly)
pka 5.94±0.10(Predicted)
form Solid
color White to Off-White
InChIKey CMJCXYNUCSMDBY-ZDUSSCGKSA-N
SMILES C(OC)(=O)N[C@@H](C)CNC1=NC=CC(C2=CN(C(C)C)N=C2C2=CC(Cl)=CC(NS(C)(=O)=O)=C2F)=N1
NCI Dictionary of Cancer Terms encorafenib
FDA UNII 8L7891MRB6
NCI Drug Dictionary encorafenib
ATC code L01EC03

SAFETY

Risk and Safety Statements

Symbol(GHS)  Exclamation Mark (GHS07)
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338
NFPA 704
0
2 0

Encorafenib (LGX818) price More Price(54)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 16994 Encorafenib ≥98% 1269440-17-6 500μg $41 2026-04-30 Buy
Cayman Chemical 16994 Encorafenib ≥98% 1269440-17-6 1mg $77 2026-04-30 Buy
Cayman Chemical 16994 Encorafenib ≥98% 1269440-17-6 5mg $180 2026-04-30 Buy
Biosynth FC65061 LGX 818 1269440-17-6 5mg $207.7 2026-06-04 Buy
Biosynth FC65061 LGX 818 1269440-17-6 10mg $324.5 2026-06-04 Buy
Product number Packaging Price Buy
16994 500μg $41 Buy
16994 1mg $77 Buy
16994 5mg $180 Buy
FC65061 5mg $207.7 Buy
FC65061 10mg $324.5 Buy

Encorafenib (LGX818) Chemical Properties, Uses, Production

Description

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.

Uses

LGX 818 is potent and selective BRAFV600E kinase inhibitor and can be used for the treatment of proliferative diseases such as solid tumor diseases.

brand name

Braftovi

General Description

Class: dual threonine/tyrosine kinase; Treatment: melanoma with BRAFV600E/K; Oral bioavailability = 85%; Elimination half-life = 6 h; Protein binding = 86%

Biological Activity

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.

Pharmacokinetics

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).
Figure 1. Putative encorafenib–BRAFV600E interactions based on BRAF inhibitor pharmacophore

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)

References

[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) synthesis

1996-30-1
1269440-17-6
Synthesis of Encorafenib (LGX818) from 2-Bromo-4-chloro-1-fluorobenzene

Encorafenib (LGX818) Preparation Products And Raw materials

Raw materials

2-((2-benzylidene-1-isopropylhydrazinyl)methylene)malononitrile CarbaMic acid, N-[(1S)-2-[[4-[3-(3-aMino-5-chloro-2-fluorophenyl)-1-(1-Methylethyl)-1H-pyrazol-4-yl]-2-pyriMidinyl]aMino]-1-Methylethyl]-, Methyl ester

Preparation Products

Encorafenib (LGX818) Suppliers

Global Suppliers ( 186)
Supplier Tel Email Country ProdList Advantage
ChengDu TongChuangYuan Pharmaceutical Co.Ltd 028-83379370 13880556291 tcy@tcypharm.com China 8696 58
Beijing Ouhe Technology Co., Ltd 13552068683 13522913783 2355560935@qq.com China 11777 60
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. 17702719238 sales@sun-shinechem.com China 1197 64
Dalian Meilun Biotech Co., Ltd. 0411-62910999 13889544652 sales@meilune.com China 4765 58
Shanghai Topbiochem Technology Co., Ltd 021-58170097 info@topbiochem.com China 9509 58
Haoyuan Chemexpress Co., Ltd. 021-58950125 info@chemexpress.com China 7545 61
MedChemexpress LLC 021-58955995 sales@medchemexpress.cn United States 4853 58
AdooQ BioScience, LLC +1 (866) 930-6790 info@adooq.com United States 2774 58
TargetMol Chemicals Inc. 021-021-33632979 15002134094 marketing@targetmol.com China 7993 58
ShangHai Caerulum Pharma Discovery Co., Ltd. 18149758185 18149758185 sales-cpd@caerulumpharma.com China 3493 58
Supplier Advantage
ChengDu TongChuangYuan Pharmaceutical Co.Ltd 58
Beijing Ouhe Technology Co., Ltd 60
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. 64
Dalian Meilun Biotech Co., Ltd. 58
Shanghai Topbiochem Technology Co., Ltd 58
Haoyuan Chemexpress Co., Ltd. 61
MedChemexpress LLC 58
AdooQ BioScience, LLC 58
TargetMol Chemicals Inc. 58
ShangHai Caerulum Pharma Discovery Co., Ltd. 58

Related articles

View Latest Price from Encorafenib (LGX818) manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Encorafenib pictures 2026-09-18 Encorafenib
1269440-17-6
 1g More Than 99% 100kg/Month BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Encorafenib pictures 2026-07-23 Encorafenib
1269440-17-6
 $47.00-124.00 99.84% 10g TargetMol Chemicals Inc.
Encorafenib (LGX818) pictures 2021-07-13 Encorafenib (LGX818)
1269440-17-6
 $10.00-15.00 1KG 99%+ HPLC Zhuozhou Wenxi import and Export Co., Ltd
  • Encorafenib pictures
  • Encorafenib
    1269440-17-6
  • $0.00
  • More Than 99%
  • BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
  • Encorafenib pictures
  • Encorafenib
    1269440-17-6
  • $47.00-124.00
  • 99.84%
  • TargetMol Chemicals Inc.

Encorafenib (LGX818) Spectrum

Encorafenib (LGX818)(1269440-17-6)1HNMR

1269440-17-6 (Encorafenib (LGX818)) Related Search:

PLX4032 Tariquidar 5-(1,1,1-Trifluoro-2-methylpropan-2-yl)isoxazol-3-amine Sorafenib Pazopanib
CEP-32496 Regorafenib Plx-4032 (RG7024) Selumetinib Dabrafenib
S3I-201 AVL-292 3-Bromo-5-chloro-2-fluoroaniline

1of3

LGX 818 CS-1037 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 Encorafenib (LGX818) 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 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]carbamate LGX818, >=98% LGX 818; LGX-818;LGX818 LGX818, Encorafenib ENCORAFENIB;LGX818; LGX-818 LGX818; LGX-818; LGX 818; ENCORAFENIB. 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)carbamate Encorafenib (LGX818) USP/EP/BP 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 NSC 4820 NSC4820 NSC-4820 Cymoxanil Impurity 3 Encorafenib, 10 mM in DMSO (S) - [1 - [[4 - [3 - [5-chloro-2-fluoro-3 - (methylsulfonamido) phenyl] - 1-isopropyl-1h-pyrazole-4-yl] pyrimidin-2-yl] amino] propyl-2-yl] carbamate 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]carbamate Encorafenib LGX818 LGX-818 1269440-17-6 C22H27ClFN7O4S Inhibitors