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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Mitogen-activated protein kinase (MAPK) >Raf inhibitors >Encorafenib (LGX818)

Encorafenib (LGX818)

Encorafenib (LGX818) Structure
  • ₹0
  • Product name: Encorafenib (LGX818)
  • CAS: 1269440-17-6
  • MF: C22H27ClFN7O4S
  • MW: 540.01
  • EINECS:
  • MDL Number:MFCD25976758
  • Synonyms: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
Manufacturer Product number Product description Packaging Price Updated Buy

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

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 Causes skin irritation Skin corrosion/irritation Category 2 Warning GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 May cause respiratory irritation Specific target organ toxicity, single exposure;Respiratory tract irritation Category 3 Warning GHS hazard pictograms
Precautionary statements:
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Description

B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling. A mutation of B-Raf in exon 15 at codon 600 where a valine is substituted by glutamic acid (V600E) has been linked to melanoma. Encorafenib is a selective inhibitor of B-RafV600E mutant melanoma cell proliferation (EC50 = 4 nM) with little activity against wild-type B-Raf or a panel of 100 other kinases (IC50s = 900 nM). At oral doses of 6 mg/kg in human melanoma xenograft models, encorafenib was shown to decrease phosphorylation of the B-Raf substrate MEK.

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