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kobe2602

Catalog No.
B3587
Ras inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$470.00
In stock
50mg
$110.00
In stock
100mg
$177.00
In stock
250mg
$320.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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].

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt419.31
Cas No.454453-49-7
FormulaC14H9F4N5O4S
Solubility≥17mg/mL in DMSO
Chemical Name2-(2,6-dinitro-4-(trifluoromethyl)phenyl)-N-(4-fluorophenyl)hydrazinecarbothioamide
SDFDownload SDF
Canonical SMILESFC1=CC=C(NC(NNC2=C([N+]([O-])=O)C=C(C(F)(F)F)C=C2[N+]([O-])=O)=S)C=C1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Chemical structure

kobe2602