kobe2602
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 419.31 |
| Cas No. | 454453-49-7 |
| Formula | C14H9F4N5O4S |
| Solubility | insoluble in H2O; ≥17 mg/mL in DMSO; ≥17.53 mg/mL in EtOH with ultrasonic |
| Chemical Name | 2-(2,6-dinitro-4-(trifluoromethyl)phenyl)-N-(4-fluorophenyl)hydrazinecarbothioamide |
| SDF | Download SDF |
| Canonical SMILES | FC1=CC=C(NC(NNC2=C([N+]([O-])=O)C=C(C(F)(F)F)C=C2[N+]([O-])=O)=S)C=C1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
