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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;LGX 818;CS-1037;NSC4820;NSC 4820;NSC-4820;LGX818, >=98%;LGX818, Encorafenib
CBNumber:
CB42668617
Molecular Formula:
C22H27ClFN7O4S
Molecular Weight:
540.01
MDL Number:
MFCD25976758
MOL File:
1269440-17-6.mol
Last updated:2024-11-19 23:02:33
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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
NCI Dictionary of Cancer Terms encorafenib
FDA UNII 8L7891MRB6
NCI Drug Dictionary encorafenib
ATC code L01EC03

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
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(27)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 16994 Encorafenib ≥98% 1269440-17-6 500μg $37 2024-03-01 Buy
Cayman Chemical 16994 Encorafenib ≥98% 1269440-17-6 1mg $70 2024-03-01 Buy
Cayman Chemical 16994 Encorafenib ≥98% 1269440-17-6 5mg $163 2024-03-01 Buy
TRC L397655 LGX818 1269440-17-6 0.5mg $90 2021-12-16 Buy
Usbiological 453725 LGX 818 1269440-17-6 500ug $368 2021-12-16 Buy
Product number Packaging Price Buy
16994 500μg $37 Buy
16994 1mg $70 Buy
16994 5mg $163 Buy
L397655 0.5mg $90 Buy
453725 500ug $368 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( 150)Suppliers
Supplier Tel Email Country ProdList Advantage
Shanghai Rochi Pharmaceutical Co.,Ltd. 		21-38751876 +8615000076078 info@rochipharma.com China 431 58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. 		+86-18600796368 +86-18600796368 sales@sjar-tech.com China 444 58
Jinan Carbotang Biotech Co.,Ltd. 		+8615866703830 figo.gao@foxmail.com China 8497 58
Hubei Jusheng Technology Co.,Ltd. 		18871490254 linda@hubeijusheng.com CHINA 28172 58
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19553 58
career henan chemical co 		+86-0371-86658258 +8613203830695 factory@coreychem.com China 29811 58
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32165 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6312 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1026@dideu.com China 22883 58
Baoji Guokang Bio-Technology Co., Ltd. 		0917-3909592 13892490616 gksales1@gk-bio.com China 9314 58
Supplier Advantage
Shanghai Rochi Pharmaceutical Co.,Ltd. 		58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. 		58
Jinan Carbotang Biotech Co.,Ltd. 		58
Hubei Jusheng Technology Co.,Ltd. 		58
BOC Sciences 		58
career henan chemical co 		58
TargetMol Chemicals Inc. 		58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		58
Dideu Industries Group Limited 		58
Baoji Guokang Bio-Technology Co., Ltd. 		58

Related articles

View Lastest Price from Encorafenib (LGX818) manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Encorafenib pictures 2024-11-19 Encorafenib
1269440-17-6
 US $47.00-124.00 / mg 99.74% 10g TargetMol Chemicals Inc.
Encorafenib pictures 2024-11-18 Encorafenib
1269440-17-6
 US $0.00 / g 1g More Than 99% 100kg/Month BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Encorafenib (LGX818) pictures 2021-07-13 Encorafenib (LGX818)
1269440-17-6
 US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
  • Encorafenib pictures
  • Encorafenib
    1269440-17-6
  • US $47.00-124.00 / mg
  • 99.74%
  • TargetMol Chemicals Inc.
  • Encorafenib pictures
  • Encorafenib
    1269440-17-6
  • US $0.00 / g
  • More Than 99%
  • BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
  • Encorafenib (LGX818) pictures
  • Encorafenib (LGX818)
    1269440-17-6
  • US $15.00-10.00 / KG
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd

Encorafenib (LGX818) Spectrum

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

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

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

1of3

LGX 818 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) 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% LGX818, Encorafenib 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 LGX 818; LGX-818;LGX818 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 LGX818 Encorafenib Cymoxanil Impurity 3 1269440-17-6 C22H27ClFN7O4S Inhibitors