Encorafenib (LGX818)

Product Name: Encorafenib (LGX818)
CAS No.: 1269440-17-6
Chemical Name: Encorafenib (LGX818)
Synonyms: Encorafenib;LGX818;CS-1037;LGX-818;LGX 818;NSC4820;NSC 4820;NSC-4820;LGX818, >=98%;LGX818, Encorafenib
CBNumber: CB42668617
Molecular Formula: C22H27ClFN7O4S
Formula Weight: 540.01
MOL File: 1269440-17-6.mol

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Encorafenib (LGX818) Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 16994
Product name: Encorafenib
Purity: ≥98%
Packaging: 500μg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 16994
Product name: Encorafenib
Purity: ≥98%
Packaging: 1mg
Price: $70
Updated: 2024/03/01

Cayman Chemical

Product number: 16994
Product name: Encorafenib
Purity: ≥98%
Packaging: 5mg
Price: $163
Updated: 2024/03/01

TRC

Product number: L397655
Product name: LGX818
Packaging: 0.5mg
Price: $90
Updated: 2021/12/16

Usbiological

Product number: 453725
Product name: LGX 818
Packaging: 500ug
Price: $368
Updated: 2021/12/16

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Encorafenib (LGX818) Chemical Properties,Usage,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).

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) Preparation Products And Raw materials

Raw materials

Preparation Products

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Encorafenib (LGX818) Suppliers

China 133 India 3 United Kingdom 1 United States 13 Global 150

MedChemexpress LLC

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ApexBio Technology

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View Lastest Price from Encorafenib (LGX818) manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.

Product: Encorafenib 1269440-17-6
Price: US $0.00/g
Min. Order: 1g
Purity: More Than 99%
Supply Ability: 100kg/Month
Release date: 2024-10-14

Zhuozhou Wenxi import and Export Co., Ltd

Product: Encorafenib (LGX818) 1269440-17-6
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-11

Zhuozhou Wenxi import and Export Co., Ltd

Product: Encorafenib (LGX818) 1269440-17-6
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-09

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

LGX 818

LGX818

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

(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

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

1269440-17-6

C22H27ClFN7O4S

Inhibitors