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Kobe0065

(CAS No:436133-68-5)
Kobe0065 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
CAS No:436133-68-5
Molecular Weight(MW):449.79
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 436133-68-5
Molecular formula(MF) C15H11ClF3N5O4S
Molecular Weight(MW): 449.79
Alias
Solubility
In vitro DMSO 89 mg/mL (197.87 mM)
Ethanol 13 mg/mL (28.9 mM)
Water <1 mg/mL
In vivo
Biological Activity
Description Kobe0065 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
Targets
H-Ras-cRaf1 interaction [1]
In vitro

Kobe0065-family compounds bind to Ras⋅GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras⋅GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition[1].

In vivo Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss[1].