918505-84-7 N-[3-[...

918505-84-7 N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide

918505-84-7 N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide

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1 Kilogram

FOB Price: USD 1000.0000

  • Min.Order :1 Kilogram
  • Purity: 99%
  • Payment Terms : L/C,T/T

Keywords

918505-84-7 N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide C17H14ClF2N3O3S

Quick Details

  • Appearance:white powder
  • Application:pharma
  • PackAge:as clients needs
  • ProductionCapacity:1|Metric Ton|Day
  • Storage:RT
  • Transportation:sea

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Details:

N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide Chemical Properties 
density  1.55 
 Safety Information 
 MSDS Information 
 N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide Usage And Synthesis 
Abstract PLX-4720 is an orally-available, ATP-competitive, highly selective, azaindole-based inhibitor of B-Raf (V600E) with IC50 value of 13 nM. PLX-4720 has additional activity towards mutant forms of c-Raf-1 (Y340D, Y341D) at an IC50 of 6.7 nM, with modest single micromolar activity versus kinases such as FRK, CSK, SRC, FGFR, KDR< HGK, and Aurora A.  PLX-4720 has shown preclinical activity in melanoma and thyroid cancer models. 
PLX-4720 preferentiallly inhibits ERK phosphorylation in tumor cell lines bearing the V600E allele. In melanoma models it induces cell cycle arrest and apoptosis exclusively in B-Raf (V600E)-positive cells.
In an orthotopic 8505c human thyroid cancer mice model, PLX-4720 caused significant reduction in tumor growth (>90%) and dramatically decreased lung metastases. 
Biological activity PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf. 
In vitro PLX-4720 displays >10 times selectivity against wild type B-Raf, and >100 times selectivity over other kinases such as Frk, Src, Fak, FGFR, and Aurora A with IC50 of 1.3-3.4 μM. PLX-4720 significantly inhibits the ERK phosphorylation in cell lines bearing B-RafV600E with IC50 of 14-46 nM, but not the cells with wild-type B-Raf. PLX-4720 significantly inhibits the growth of tumor cell lines bearing the B-RafV600E oncogene, such as COLO205, A375, WM2664, and COLO829 with GI50 of 0.31 μM, 0.50 μM, 1.5 μM, and 1.7 μM, respectively. In addition, PLX-4720 treatment at 1 μM induces cell cycle arrest and apoptosis exclusively in the B-RafV600E-positive 1205Lu cells, but not in the B-Raf wild-type C8161 cells. 
 
 
 
 

 

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