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
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
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.
N-Bromosuccinimide Price
- Product number
- 16994
- Product name
- Encorafenib
- Purity
- ≥98%
- Packaging
- 500μg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 16994
- Product name
- Encorafenib
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $70
- Updated
- 2024/03/01
- Product number
- 16994
- Product name
- Encorafenib
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $163
- Updated
- 2024/03/01
- Product number
- L397655
- Product name
- LGX818
- Packaging
- 0.5mg
- Price
- $90
- Updated
- 2021/12/16
- Product number
- 453725
- Product name
- LGX 818
- Packaging
- 500ug
- Price
- $368
- Updated
- 2021/12/16
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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View Lastest Price from Encorafenib (LGX818) manufacturers
- 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
- 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
- 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