KOBE2602,

KOBE2602,

KOBE2602,

Min.Order / FOB Price:Get Latest Price

100 Gram

FOB Price: USD 1.0000

  • Min.Order :100 Gram
  • Purity: 98%
  • Payment Terms : L/C

Keywords

KOBE2602, kobe 2602;kobe2602;kobe-2602;2-[2,6-Dinitro-4-(trifluoroMethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioaMide;kobe-2602 2-[2,6-Dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothi 454453-49-7

Quick Details

  • Appearance:White crystal
  • Application:CAS:454453-49-7; Aromatics, Miscellaneous Reagents, Pharmaceuticals, Intermediates & Fine Chemicals;Inhibitors;
  • PackAge:100g,500g,1kg,25kg/drum
  • ProductionCapacity:1000|Gram|Week
  • Storage:Dry seal
  • Transportation:shipping

Superiority:

We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.
 
 
 
We are committed to provide excellence in researching, manufacturing and drug discovery process.
 
 
 
Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.

 

Details:

kobe2602 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 149 ± 55 μM.
IC50 value: 149 ± 55 uM (Ki) [1]
Target: Ras-Raf
These two compounds(Kobe0065 and Kobe2602), added to the culture medium at 2 and 20 μM, effectively reduced the amount of c-Raf-1 associated with H-Ras G12V in NIH 3T3 cells in a dose-dependent manner, indicating the inhibition of the cellular activity of Ras. A rough estimate of the IC50 value for the cellular Ras–Raf-binding inhibition was around 10 μM (Fig. 1B), which was not much different from the Ki values for the in vitro Ras–Raf-binding inhibition considering thequite low cellular concentration of Raf. A similar inhibitory effect was also observed with NIH 3T3 cells overexpressing K-Ras G12V. Both Kobe0065 and Kobe2602 at 20 μM efficiently inhibited the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-Ras G12V, although the effect was slightly weaker than that of 2 μM sorafenib.

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