Chemical Structure : Kobe2602
CAS No.: 454453-49-7
Catalog No.: PC-21604Not For Human Use, Lab Use Only.
Kobe2602 is a small-molecule Ras inhibitor that display antitumor activity by interfering with Ras·GTP-effector interaction, inhibits the binding of H-Ras⋅GTP to c-Raf-1 RBD with Ki of 149 uM.
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Kobe2602 is a small-molecule Ras inhibitor that display antitumor activity by interfering with Ras·GTP-effector interaction, inhibits the binding of H-Ras⋅GTP to c-Raf-1 RBD with Ki of 149 uM.
Kobe2602 (20 μM) efficiently inhibited the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-RasG12V.
Kobe2602 (20 μM) almost completely inhibited the proliferation of H-rasG12V–transformed NIH 3T3 cells in the presence of 2% FBS (IC50=2 uM).
Kobe2602 (80 mg/kg) exhibited antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-rasG12V gene by oral administration.
M.Wt | 419.31 | |
Formula | C14H9F4N5O4S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
2-(2,6-Dinitro-4-(trifluoromethyl)phenyl)-N-(4-fluorophenyl)hydrazine-1-carbothioamide |
1. Shima F, et al. Proc Natl Acad Sci U S A. 2013 May 14;110(20):8182-7.
2. Shima F, et al. Enzymes. 2013;34 Pt. B:1-23.
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