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Encorafenib (LGX818)

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Company Name: Shanghai Rochi Pharmaceutical Co.,Ltd.
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CAS:1269440-17-6
Purity:99%min
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CAS:1269440-17-6
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CAS:1269440-17-6
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Company Name: BOC Sciences
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CAS:1269440-17-6
Purity:>=98% Package:150mg Remarks:BOC Sciences also provides custom synthesis services for Encorafenib.
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CAS:1269440-17-6
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Encorafenib (LGX818) manufacturers

  • Encorafenib (LGX818)
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  • $15.00 / 1KG
  • 2021-07-13
  • CAS:1269440-17-6
  • Min. Order: 1KG
  • Purity: 99%+ HPLC
  • Supply Ability: Monthly supply of 1 ton
  • Encorafenib (LGX818)
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  • $15.00 / 1KG
  • 2021-07-10
  • CAS:1269440-17-6
  • Min. Order: 1KG
  • Purity: 99%+ HPLC
  • Supply Ability: Monthly supply of 1 ton
  • Encorafenib (LGX818)
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  • $6.60 / 1KG
  • 2019-12-26
  • CAS:1269440-17-6
  • Min. Order: 1KG
  • Purity: 97%-99%
  • Supply Ability: 1kg-1000kg

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Encorafenib (LGX818) Basic information
Product Name:Encorafenib (LGX818)
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
CAS:1269440-17-6
MF:C22H27ClFN7O4S
MW:540.01
EINECS:
Product Categories:Inhibitors
Mol File:1269440-17-6.mol
Encorafenib (LGX818) Structure
Encorafenib (LGX818) Chemical 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)
pka5.94±0.10(Predicted)
form Solid
color White to Off-White
Safety Information
MSDS Information
Encorafenib (LGX818) Usage And Synthesis
DescriptionEncorafenib (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.
UsesLGX 818 is potent and selective BRAFV600E kinase inhibitor and can be used for the treatment of proliferative diseases such as solid tumor diseases.
Biological ActivityEncorafenib (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.
Clinical UseEncorafenib (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.
targetB-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.
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