kobe-2602 Chemical Properties

Boiling point:

450.8±55.0 °C(Predicted)

Density 

1.691±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

insoluble in H2O; ≥17 mg/mL in DMSO; ≥17.53 mg/mL in EtOH with ultrasonic

form 

solid

pka

9.35±0.70(Predicted)

color 

Light yellow to brown

kobe-2602 Usage And Synthesis

Uses

2-[2,6-Dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioamide is used in the preparation of pyrazolidine or pyrazole compounds which exhibit mild antimicrobial effects against various strains of bacteria.

Uses

Kobe 2602 is used in the preparation of pyrazolidine or pyrazole compounds which exhibit mild antimicrobial effects against various strains of bacteria.

Biological Activity

kobe2602 is a small-molecule inhibitor of ras with ki value of 149 μm [1].kobe2602 is a compound screened out by a computer-assisted search of about 160,000 compounds. it dose-dependently inhibited the binding of h-rasg12v to c-raf-1 in nih 3t3 cells with a rough ic50 value of 10 μm. 20 μm of kobe2602 effectively suppressed the phosphorylation of down-stream kinases of raf, including mek and erk. besides that, in nih 3t3 cells transfected with h-rasg12v, kobe2602 inhibited the colony formation with ic50 value of 1.4 μm. kobe2602 also showed effect on other cancer cells carrying activated ras oncogenes, such as panc-1(k-rasg12v), ht1080 (n-rasq61l) and hct116 (h-rasg13d). moreover, in mice bearing sw480 xenografts, administration of kobe2602 resulted in 40-50% inhibition of the tumor growth at dose of 80 mg/kg [1].

in vivo

References

[1] shima f, yoshikawa y, ye m, et al. in silico discovery of small-molecule ras inhibitors that display antitumor activity by blocking the ras–effector interaction. proceedings of the national academy of sciences, 2013, 110(20): 8182-8187.